Cyclic ketone compound and medical effect thereof

Abstract

The present invention relates to the technical field of anesthetic drugs, and provides a cyclic ketone compound and a medical effect thereof. The cyclic ketone compound of the present invention is a compound represented by formula (I), or a stereoisomer thereof, or a deuterated derivative thereof, or a prodrug thereof, or a salt thereof, or a solvate thereof. According to the present invention, it is found that the cyclic ketone compound and the prodrug thereof can significantly ameliorate respiratory depression caused by anesthetic and / or sedative drugs, and can improve the respiratory function during inhalation general anesthesia in which spontaneous respiration is retained; additionally, compared with sodium camphorsulfonate and oxocamphor, the compound of the present invention can significantly ameliorate opioid-induced respiratory depression at lower doses, and has a higher minimum dose inducing adverse reactions and better safety. The present invention has a good amelioration effect on respiratory depression caused by opioid drugs and inhalation anesthetics, provides a new solution for respiratory depression caused by clinical anesthesia, and has wide application prospects.

Description

A cyclic ketone compound and its medical effects Technical Field

[0001] The present invention belongs to the technical field of anesthetic drugs, and in particular relates to a cyclic ketone compound and its medical effects. Background Art

[0002] General anesthetics, also known as general anesthetics, are a class of drugs that can inhibit the function of the central nervous system. They can reversibly cause loss of consciousness, sensation, and reflexes, and relaxation of skeletal muscles. They are mainly used for surgical anesthesia. Postoperative anesthesia recovery time has always been one of the issues of clinical concern, and it is closely related to a variety of factors. Prolonged postoperative anesthesia recovery time will increase the patient's endotracheal intubation time, prolong the patient's exposure to the risks of general anesthesia, increase the incidence of cardiovascular and pulmonary complications, and affect the prognosis of surgical patients. In addition, prolonged anesthesia recovery time will greatly reduce the utilization efficiency of the operating room, increase the vacancy rate of the operating room, and increase the cost for patients and medical staff. Moreover, with the update of the concept of day surgery, rapid anesthesia recovery and good recovery quality are the cornerstones of promoting day surgery and ensuring the safety of day surgery.

[0003] With increasing demands for surgical safety and controllability, antagonists for some anesthetic drugs have emerged, such as the opioid antagonist naloxone, the broad-spectrum muscle relaxant antagonist neostigmine, and the muscle relaxant rocuronium bromide-specific antagonist sugammadex. These antagonists can rapidly reverse the anesthetic effects of opioids or muscle relaxants, facilitating patient recovery and reversing anesthetic effects in emergency situations. However, there is currently a lack of methods and approaches to address delayed recovery from prolonged infusions of general anesthetics and to reverse the effects of general anesthetics in emergency situations.

[0004] Currently, the drug with clear antagonistic effect used in clinical practice is flumazenil. Specific antagonists of benzodiazepines can reverse However, studies have shown that flumazenil has no significant antagonistic effect on the anesthesia induced by propofol. These drugs are no longer routinely used in clinical anesthesia, and there is an urgent need to develop broader-spectrum antagonists, especially those covering common general anesthetics such as propofol and etomidate.

[0005] Summary of the Invention

[0006] The object of the present invention is to provide a cyclic ketone compound and its medical effects. The cyclic ketone compound of the present invention can be used to prepare anesthetic and / or sedative antagonist drugs.

[0007] The present invention provides a compound represented by Formula I, or a stereoisomer thereof, or a deuterated derivative thereof, or a prodrug thereof, or a salt thereof, or a solvate thereof:

[0008] in,

[0009] n1 is 1 or 2;

[0010] n is 0, 1 or 2; when n is 0, the connection between R6 and R4 and the connection between R3 and R4 If not, connect R6 and R3 When n is 1 or 2, the bond connecting R6 and R4 and the bond connecting R3 and R4 As a key, connect R6 and R3 is a key or None;

[0011] m is 0 or 1; when m is 0, the connection between R8 and R0 and the connection between R8 and R3 When m is 1, R8 and R0 are connected, and R8 and R3 are connected. is the key;

[0012] Connect R3, R 10 , R7, R 11 of According to the number of bonds connecting carbon atoms, it is bonded or absent;

[0013] R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 、-CR 12 =NR 13 、-CR 12 R 13 NR 14 R 15 、-NR 13 CSR12 、-CONR 12 R 13 The substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0014] R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form =NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring;

[0015] L1, L2, L3, L4, and L5 are each independently selected from the following groups: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0016] R x1 、R x2 、R x3 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x1 、R x2 、R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0017] R 11 Selected from hydrogen, deuterium, tritium, halogen, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl;

[0018] R3, R 10 Each independently selected from -L6L7L8R x4 ;

[0019] L6, L7, L8 are each independently selected from the following groups: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0020] R x4 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0021] R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , =C(L 12 R X6 )(L 13 R X7 ), =O; or R4 and R5 or R6 and R7 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carboheterocyclic ring;

[0022] L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0023] R x5 、R x6 、R x7 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x5 、R x6 、R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0024] R8 and R9 are each independently selected from -L 14 L 15 L 16 R X8 ;

[0025] L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; said L 14 , L 15 , L 16The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0026] R x8 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x8 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0027] R 12 、R 13 、R 14 、R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, and 3- to 10-membered heterocycloalkyl.

[0028] Furthermore, the compound is represented by Formula II:

[0029] in,

[0030] n is 0, 1 or 2; when n is 0, the connection between R6 and R4 and the connection between R3 and R4 If not, connect R6 and R3 When n is 1 or 2, the bond connecting R6 and R4 and the bond connecting R3 and R4 As a key, connect R6 and R3 is a key or None;

[0031] Connect R 10 、R7 According to the number of bonds connecting carbon atoms, it is bonded or absent;

[0032] R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 、-CR 12 =NR 13 、-CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0033] R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form =NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring;

[0034] L1, L2, L3, L4, and L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0035] R x1 、R x2 、R x3 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x1 、R x2 、R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0036] R 11 Selected from hydrogen, deuterium, tritium, halogen, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl;

[0037] R3, R 10 Each independently selected from -L6L7L8R x4 ;

[0038] L6, L7, L8 are each independently selected from the following groups: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、 -CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0039] R x4 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0040] R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , =C(L 12 R X6 )(L 13 R X7), =O; or R4 and R5 or R6 and R7 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carboheterocyclic ring;

[0041] L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0042] R x5 、R x6 、R x7 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x5 、R x6 、R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0043] R 12 、R 13 、R 14 、R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl;

[0044] Preferably, the compound is represented by formula II-1 or II-2:

[0045] Furthermore, the compound is represented by formula III:

[0046] in,

[0047] n is 0, 1 or 2; when n is 0, the connection between R6 and R4 and the connection between R3 and R4 If not, connect R6 and R3 When n is 1 or 2, the bond connecting R6 and R4 and the bond connecting R3 and R4 As a key, connect R6 and R3 is a key or None;

[0048] Connect R3 and R7 According to the number of bonds connecting carbon atoms, it is bonded or absent;

[0049] R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 、-CR 12 =NR 13、-CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0050] R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form =NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring;

[0051] L1, L2, L3, L4, and L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl;

[0052] R x1 、R x2 、R x3Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x1 、R x2 、R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0053] R3 is selected from -L6L7L8R x4 ;

[0054] L6, L7, L8 are each independently selected from the following groups: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0055] R x4 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0056] R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , =C(L 12 R X6 )(L 13 R X7 ), =O; or R4 and R5 or R6 and R7 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carboheterocyclic ring;

[0057] L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0058] R x5 、R x6 、R x7 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x5 、R x6 、R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0059] R8 and R9 are each independently selected from -L 14 L 15 L 16 R X8 ;

[0060] L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; said L 14 , L 15 , L 16The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0061] R x8 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x8 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0062] R 12 、R 13 、R 14 、R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, and 3- to 10-membered heterocycloalkyl.

[0063] Furthermore, the compound is represented by Formula IIIa or Formula IIIb:

[0064] in,

[0065] n, R0, R1, R2, R3, R4, R5, R6, R7, R8, and R9 are as shown above.

[0066] Furthermore, the compound is represented by Formula IIa:

[0067] in,

[0068] R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 、-CR 12 =NR 13 、-CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0069] R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form =NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring;

[0070] L1, L2, L3, L4, and L5 are each independently selected from the following groups: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0071] R x1 、R x2 、R x3 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x1 、R x2 、R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0072] R 11 Selected from hydrogen, deuterium, tritium, halogen, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl;

[0073] R3 is selected from -L6L7L8R x4 ;

[0074] L6, L7, L8 are each independently selected from the following groups: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0075] R x4 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0076] R6 is selected from -L9L 10 L 11 R X5 ;

[0077] L9, L 10 , L 11 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR14 -; L9, L 10 , L 11 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0078] R x5 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x5 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0079] R 12 、R 13 、R 14 、R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl;

[0080] Preferably, the compound is represented by Formula IIa-1 or Formula IIa-2:

[0081] Furthermore, the compound is represented by formula IIIa:

[0082] in,

[0083] R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, COR 12、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 、-CR 12 =NR 13 、-CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0084] R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form =NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring;

[0085] L1, L2, L3, L4, and L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14-; the substituents in L1, L2, L3, L4, and L5 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0086] R x1 、R x2 、R x3 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x1 、R x2 、R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0087] R6 is selected from -L9L 10 L 11 R X5 ;

[0088] L9, L 10 , L 11 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L10 , L 11 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0089] R x5 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x5 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0090] R8 and R9 are each independently selected from -L 14 L 15 L 16 R X8 ;

[0091] L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; said L 14 , L 15 , L16 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0092] R x8 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x8 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0093] R 12 、R 13 、R 14 、R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, and 3- to 10-membered heterocycloalkyl.

[0094] Furthermore, the compound is represented by Formula IIIa1 or Formula IIIa2:

[0095] Among them, R0, R1, R2, R6, R8, and R9 are as shown above.

[0096] Furthermore, the compound is represented by Formula IIb:

[0097] in,

[0098] R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, COR12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 、-CR 12 =NR 13 、-CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0099] R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form =NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring;

[0100] L1, L2, L3, L4, and L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR14 -; the substituents in L1, L2, L3, L4, and L5 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl;

[0101] R x1 、R x2 、R x3 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x1 、R x2 、R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0102] R 11 Selected from hydrogen, deuterium, tritium, halogen, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl;

[0103] R3, R 10 Each independently selected from -L6L7L8R x4 ;

[0104] L6, L7, L8 are each independently selected from the following groups: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12=N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0105] R x4 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0106] R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , =C(L 12 R X6 )(L 13 R X7 ), =O; or R4 and R5 or R6 and R7 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carboheterocyclic ring;

[0107] L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0108] R x5 、R x6 、R x7 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x5 、R x6 、R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0109] R 12 、R 13 、R 14 、R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl;

[0110] Preferably, the compound is represented by Formula IIb-1, Formula IIb-2, Formula IIb-3 or Formula IIb-4:

[0111] Furthermore, the compound is represented by formula IIIb:

[0112] in,

[0113] R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 、-CR 12 =NR 13 、-CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0114] R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form =NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring;

[0115] L1, L2, L3, L4, and L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0116] R x1 、R x2 、R x3 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x1 、R x2 、R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0117] R3 is selected from -L6L7L8R x4 ;

[0118] L6, L7, L8 are each independently selected from the following groups: C1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0119] R x4 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0120] R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , =C(L 12 R X6 )(L 13 R X7 ), =O; or R4 and R5 or R6 and R7 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carboheterocyclic ring;

[0121] L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0122] R x5 、R x6 、R x7 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x5 、R x6 、R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0123] R8 and R9 are each independently selected from -L14 L 15 L 16 R X8 ;

[0124] L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; said L 14 , L 15 , L 16 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0125] R x8 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x8 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0126] R 12 、R 13 、R14 、R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, and 3- to 10-membered heterocycloalkyl.

[0127] Furthermore, the compound is represented by formula IIIb1 or IIIb2:

[0128] in,

[0129] R0, R1, R2, R3, R4, R5, R6, R7, R8, and R9 are as shown above.

[0130] Furthermore, the compound is represented by Formula IIa1:

[0131] in,

[0132] R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 、-CR 12 =NR 13 、-CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0133] R 11 Selected from hydrogen, deuterium, tritium, halogen, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl;

[0134] R3 is selected from -L6L7L8R x4 ;

[0135] L6, L7, L8 are each independently selected from the following groups: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0136] R x4 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0137] R6 is selected from -L9L 10 L 11 R X5 ;

[0138] L9, L 10 , L 11 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0139] R x5 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x5 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0140] R 12 、R 13 、R 14 、R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl;

[0141] Preferably, the compound is represented by formula IIa1-1 or IIa1-2:

[0142] Furthermore,

[0143] R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl; the substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, and nitro;

[0144] R 11 Selected from hydrogen, deuterium, tritium, and halogen;

[0145] R3 is selected from -L6L7L8R x4 ;

[0146] L6, L7, L8 are each independently selected from the following groups: C 1～6 Alkylene, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, -CO-, -NR 13 -、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 alkoxy;

[0147] R x4 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 alkyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5Alkyl, C 1～5 alkoxy;

[0148] R6 is selected from -L9L 10 L 11 R X5 ;

[0149] L9, L 10 , L 11 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, -CO-, -COO-, -OCO-, -O-, -S-, -SOO-, -NR 13 -、-CONR 13 -; L9, L 10 , L 11 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 alkoxy;

[0150] R x5 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 alkenyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl; the R x5 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 alkoxy;

[0151] R 12 、R 13 、R 14 、R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Furthermore, the compound is represented by Formula IIb1, IIb2 or IIb3:

[0152] in,

[0153] R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 、-CR 12 =NR 13 、-CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0154] R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form =NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring;

[0155] L1, L2, L3, L4, and L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0156] R x1 、R x2 、R x3 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x1 、R x2 、R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0157] R 11 Selected from hydrogen, deuterium, tritium, halogen, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl;

[0158] R3, R 10 Each independently selected from -L6L7L8R x4 ;

[0159] L6, L7, L8 are each independently selected from the following groups: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0160] R x4 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0161] R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , =C(L 12 R X6 )(L 13 R X7 ), =O; or R4 and R5 or R6 and R7 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carboheterocyclic ring;

[0162] L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0163] R x5 、R x6 、R x7 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x5 、R x6 、R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0164] R 12 、R 13 、R 14 、R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl;

[0165] Preferably, the compound is represented by formula IIb1-1, IIb1-2, IIb2-1, IIb2-2, IIb3-1, or IIb3-2:

[0166] Furthermore,

[0167] R0 is selected from the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl; the substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, and nitro;

[0168] R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form =NL3R X1 , =C(L4R X2 )(L5R X3 ); or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carboheterocyclic ring;

[0169] L1, L2, L3, L4, and L5 are each independently selected from the following groups: C 1～6 Alkylene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -O-, -S-, -SOO-, -NR 13 CO-、 -NR 13 -、-CONR 13 -; the substituents in L1, L2, L3, L4, and L5 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 alkoxy;

[0170] R x1 、R x2 、R x3 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 alkyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl; the R x1 、R x2 、R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 alkoxy;

[0171] R 11 Selected from hydrogen, deuterium, tritium, and halogen;

[0172] R3, R 10 Each independently selected from -L6L7L8R x4 ;

[0173] L6, L7, L8 are each independently selected from the following groups: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -NR 13 -、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 alkoxy;

[0174] R x4 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 alkoxy;

[0175] R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , =C(L 12 R X6 )(L 13 R X7 );

[0176] L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6Alkylene, -CO-, -COO-, -OCO-, -O-, -S-, -SOO-, -NR 13 -、-CONR 13 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 alkoxy;

[0177] R x5 、R x6 、R x7 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 6-10 membered aryl; said R x5 、R x6 、R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 alkoxy;

[0178] R 12 、R 13 、R 14 、R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy.

[0179] Furthermore, the compound is represented by Formula IIIb1, IIIb2 or IIIb3:

[0180] in,

[0181] R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12-、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 、-CR 12 =NR 13 、-CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0182] R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form =NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring;

[0183] L1, L2, L3, L4, and L5 are each independently selected from the following groups: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0184] R x1 、R x2 、R x3 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x1 、R x2 、R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0185] R3 is selected from -L6L7L8R x4 ;

[0186] L6, L7, L8 are each independently selected from the following groups: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0187] R x4 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0188] R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , =C(L 12 R X6 )(L 13 R X7 ), =O; or R4 and R5 or R6 and R7 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carboheterocyclic ring;

[0189] L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0190] R x5 、R x6 、R x7 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x5 、R x6 、R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0191] R8 and R9 are each independently selected from -L 14 L 15 L 16 R X8 ;

[0192] L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR12 R 13 NR 14 -; said L 14 , L 15 , L 16 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0193] R x8 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x8 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0194] R 12 、R 13 、R 14 、R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, and 3- to 10-membered heterocycloalkyl.

[0195] Furthermore, the compound is represented by Formula IIIb11, Formula IIIb12, Formula IIIb21, Formula IIIb22, Formula IIIb31 or Formula IIIb32:

[0196] in,

[0197] R0, R1, R2, R3, R4, R5, R6, R7, R8, and R9 are as shown above.

[0198] Furthermore,

[0199] R0 is selected from the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl; the substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, and nitro;

[0200] R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form =NL3R X1 , =C(L4R X2 )(L5R X3 ); or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carboheterocyclic ring;

[0201] L1, L2, L3, L4, and L5 are each independently selected from the following groups: C 1～6 Alkylene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -O-, -S-, -SOO-, -NR 13 CO-、-NR 13 -、-CONR 13 -; the substituents in L1, L2, L3, L4, and L5 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0202] R x1 、R x2 、R x3 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 alkyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl; the R x1 、R x2 、R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0203] R3 is selected from -L6L7L8R x4 ;

[0204] L6, L7, L8 are each independently selected from the following groups: C 1～6 Alkylene, C2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -CONR 13 -、-NR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0205] R x4 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0206] R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , =C(L 12 R X6 )(L 13 R X7 );

[0207] L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, -CO-, -COO-, -OCO-, -O-, -S-, -SOO-, -NR 13 -、-CONR 13 -; L9, L 10 , L 11 , L 12 , L13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0208] R x5 、R x6 、R x7 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 6-10 membered aryl; said R x5 、R x6 、R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0209] R8 and R9 are each independently selected from -L 14 L 15 L 16 R X8 ;

[0210] L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl; said L 14 , L 15 , L 16 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0211] R x8 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy; the R x8The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0212] R 12 、R 13 、R 14 、R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, and 3- to 10-membered heterocycloalkyl.

[0213] Further, the compound is not:

[0214] Furthermore, the compound is represented by Formula IV:

[0215] in,

[0216] R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, COR 12 、-COOR 12 、 -OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 、-CR 12 =NR 13 、-CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12、-CONR 12 R 13 The substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0217] R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form =NL3R X1 , =C(L4R X2 )(L5R X3 ); or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carboheterocyclic ring;

[0218] L1, L2, L3, L4, and L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0219] R x1 、R x2 、R x3 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x1 、R x2 、R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0220] R 12 、R 13 、R 14 、R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl;

[0221] The compound is not:

[0222] Preferably,

[0223] in,

[0224] R0 is selected from C 1～6 alkyl;

[0225] R1 is selected from hydrogen, deuterium, tritium, C 1～6 alkyl;

[0226] R2 is selected from -L1L2L3R X1 ;

[0227] L1, L2, L3 are each independently selected from none, -CO-, -O-, -SOO-, unsubstituted or substituted with one or two or more substituents C 1～6 Alkylene; the substituents in L1, L2, and L3 are each independently selected from hydroxyl groups;

[0228] R x1 Selected from C 1～6 Alkyl, 3-10 membered cycloalkyl, 5-10 membered heteroaryl, unsubstituted or substituted with one or two or more substituents 6-10 membered aryl; said R x1 The substituents in are independently selected from halogen, C 1～5 Alkyl, C1～5 Alkoxy.

[0229] Furthermore, the compound is represented by Formula IVa or Formula IVb:

[0230] Among them, R0, R1, and R2 are as shown above.

[0231] Furthermore,

[0232] -L1L2L3R X1 In the embodiment, the structure of -L1L2L3- is selected from none,

[0233] R x1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, 3-6 membered cycloalkyl, thienyl, phenyl which is unsubstituted or substituted with one or two or more substituents; said R x1 The substituents in each of the groups are independently selected from fluorine, chlorine, bromine, iodine, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, C 1～5 Alkoxy.

[0234] Furthermore, the compound is one of the following compounds:

[0235] Furthermore, the compound is represented by Formula V:

[0236] in,

[0237] R0 is selected from C 1～6 alkyl;

[0238] R3 is selected from -L6L7L8R x4 ;

[0239] L6, L7, L8 are each independently selected from none, C 1～6 Alkylene, -CO-, -NR 13 -;

[0240] R x4 Selected from the following groups: fluorine, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl; the R x4 The substituents in are each independently selected from C 1～5 Alkyl; and when L6, L7, and L8 are all null, R x4 Not selected from methyl;

[0241] R 13Selected from hydrogen, deuterium, tritium, C 1～6 alkyl.

[0242] Furthermore, the compound is represented by Formula Va or Formula Vb:

[0243] Among them, R0 and R3 are as shown above.

[0244] Furthermore,

[0245] -L6L7L8R x4 In the embodiment, the structure of -L6L7L8- is selected from the group consisting of:

[0246] R x4 Selected from the following groups: fluorine, unsubstituted or substituted by one or two or more substituents: methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, 3-6 membered cycloalkyl, The R x4 The substituents in -L6L7L8R are each independently selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl; and x4 When there is no x4 Not selected from methyl;

[0247] R 13 is selected from hydrogen, deuterium, tritium, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, and tert-butyl.

[0248] Furthermore, the compound is one of the following compounds:

[0249] Furthermore, the compound is represented by Formula VIa or VIb:

[0250] in,

[0251] R0 is selected from hydrogen, deuterium, tritium, F, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl; the substituents in R0 are each independently selected from hydrogen, deuterium, tritium, F, I, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 alkoxy;

[0252] R 11 Selected from hydrogen, deuterium, tritium, F, I, C 1～6Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl;

[0253] R3, R 10 Each independently selected from -L6L7L8R x4 ;

[0254] L6, L7, L8 are each independently selected from the following groups: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0255] R x4 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0256] R 12 、R 13 、R 14are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl;

[0257] The compound is not:

[0258] Preferably,

[0259] in,

[0260] R0 is selected from fluorine, C 1～6 alkyl;

[0261] R 11 Selected from fluorine, C 1～6 alkyl;

[0262] R3, R 10 Each independently selected from -L6L7L8R x4 ;

[0263] -L6L7L8R x4 In the formula, the structure of -L6L7L8- is selected from none;

[0264] R x4 Selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 2～6 alkenyl, 3-6 membered cycloalkyl; and R3, R 10 R in x4 Not simultaneously hydrogen;

[0265] Preferably, the compound is represented by Formula VIa-1, VIa-2, VIb-1 or VIb-2:

[0266] Furthermore,

[0267] R0 is selected from fluorine, methyl;

[0268] R 11 Selected from fluorine, methyl;

[0269] R3, R 10 Each independently selected from -L6L7L8R x4 ;

[0270] -L6L7L8R x4 In the formula, the structure of -L6L7L8- is selected from none;

[0271] R x4 is selected from hydrogen, deuterium, tritium, methyl, isopropyl, cyclopropyl, isopropenyl; and R3, R 10R in x4 Not hydrogen at the same time.

[0272] Furthermore, the compound is one of the following compounds:

[0273] Furthermore, the compound is represented by Formula VIIa or VIIb:

[0274] in,

[0275] R0 is selected from the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl; the substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, and nitro;

[0276] R 11 Selected from hydrogen, deuterium, tritium, F, I, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl;

[0277] R3 is selected from -L6L7L8R x4 ;

[0278] L6, L7, L8 are each independently selected from the following groups: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0279] R x4A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0280] R 12 、R 13 、R 14 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl;

[0281] The compound is not:

[0282] Preferably,

[0283] in,

[0284] R0 is selected from fluorine, C 1～6 alkyl;

[0285] R 11 Selected from fluorine, C 1～6 alkyl;

[0286] R3 is selected from -L6L7L8R x4 ;

[0287] -L6L7L8R x4 In the formula, the structure of -L6L7L8- is selected from none;

[0288] R x4 Selected from C 1～6 alkyl;

[0289] More preferably, the compound is represented by Formula VIIa-1, VIIa-2, VIIb-1 or VIIb-2:

[0290] Furthermore,

[0291] R0 is selected from fluorine, methyl;

[0292] R 11 Selected from fluorine, methyl;

[0293] R3 is selected from -L6L7L8R x4 ;

[0294] -L6L7L8R x4 In the formula, the structure of -L6L7L8- is selected from none;

[0295] R x4 Selected from isopropyl.

[0296] Furthermore, the compound is one of the following compounds:

[0297] Furthermore, the compound is represented by Formula VIII:

[0298] in,

[0299] R0 is selected from the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl; the substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, and nitro;

[0300] R9 is selected from -L 14 L 15 L 16 R X8 ;

[0301] L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; said L 14 , L 15 , L16 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0302] R x8 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x8 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0303] R 12 、R 13 、R 14 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl;

[0304] The compound is not:

[0305] Preferably,

[0306] in,

[0307] R0 is selected from C 1～6 alkyl;

[0308] R9 is selected from -L 14 L 15 L 16 R X8 ;

[0309] L 14 , L 15 , L 16 Each independently selected from none, -O-, -CO-, -SOO-, unsubstituted or substituted by one or two or more substituents C 1～6 Alkylene; said L 14 , L15 , L 16 The substituents in are each independently selected from hydroxyl groups;

[0310] R x8 Selected from C 1～6 Alkyl, 3-10 membered cycloalkyl, unsubstituted or substituted by one or two or more substituents phenyl; said R x8 The substituents in are independently selected from halogen, C 1～5 Alkyl, C 1～5 Alkoxy.

[0311] Furthermore, the compound is represented by Formula VIIIa or VIIIb:

[0312] Among them, R0 and R9 are as shown above.

[0313] Furthermore,

[0314] -L 14 L 15 L 16 R X8 -L 14 L 15 L 16 -The structure is selected from none,

[0315] R X8 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, 3-6 membered cycloalkyl, phenyl which is unsubstituted or substituted with one or two or more substituents; said R x8 The substituents in each of the groups are independently selected from fluorine, chlorine, bromine, iodine, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, C 1～5 Alkoxy.

[0316] Furthermore, the compound is one of the following compounds:

[0317] Furthermore, the compound is represented by Formula IX:

[0318] in,

[0319] R0 is selected from the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl; the substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, and nitro;

[0320] R3 is selected from -L6L7L8R x4 ;

[0321] L6, L7, L8 are each independently selected from the following groups: C 1～6 Alkylene, C 3～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 7-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0322] R x4 A group selected from hydrogen, deuterium, tritium, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 7-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x4 The substituents in are independently selected from hydrogen, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0323] R 12 、R 13 、R 14 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl;

[0324] The compound is not:

[0325] Preferably,

[0326] in,

[0327] R0 is selected from C 1～6 alkyl;

[0328] R3 is selected from -L6L7L8R x4 ;

[0329] L6, L7, L8 are each independently selected from none, C 1～6 Alkylene, -CO-, -NR 13 -;

[0330] R x4 Selected from 3-10 membered cycloalkyl, C 1～6 alkyl.

[0331] Furthermore, the compound is represented by Formula IXa or Formula IXb:

[0332] Among them, R0 and R3 are as shown above.

[0333] Furthermore,

[0334] -L6L7L8R x4 In the embodiment, the structure of -L6L7L8- is selected from the group consisting of:

[0335] R x4 Selected from 3-6 membered cycloalkyl, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl and tert-butyl.

[0336] Furthermore, the compound is one of the following compounds:

[0337] Furthermore, the compound is represented by formula X:

[0338] in,

[0339] R0 is selected from the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl; the substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, and nitro;

[0340] R9 is selected from -L 14 L 15 L 16 R X8 ;

[0341] L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; said L 14 , L 15 , L 16 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0342] R x8 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x8 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0343] R 12 、R 13 、R 14 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl;

[0344] The compound is not:

[0345] Preferably,

[0346] R0 is selected from C 1～6 alkyl;

[0347] R9 is selected from -L 14 L 15 L 16 R X8 ;

[0348] L 14 , L 15 , L 16 Each independently selected from none, -CO-, -O-, -SOO-, unsubstituted or substituted by one or two or more substituents C 1～6 Alkylene; said L 14 , L 15 , L 16 The substituents in are each independently selected from hydroxyl groups;

[0349] R x8 Selected from C 1～6 Alkyl, 3-6 membered cycloalkyl, unsubstituted or substituted by one or two or more substituents phenyl; said R x8 The substituents in are independently selected from fluorine, chlorine, bromine, iodine, C 1～5 Alkyl, C 1～5 Alkoxy.

[0350] Furthermore, the compound is represented by Formula Xa or Formula Xb:

[0351] Among them, R0 and R9 are as shown above.

[0352] Furthermore,

[0353] -L 14 L 15 L 16 R X8 -L 14 L 15 L 16 -The structure is selected from none,

[0354] R X8 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, 3-6 membered cycloalkyl, phenyl which is unsubstituted or substituted with one or two or more substituents; said R x8The substituents in each of the groups are independently selected from fluorine, chlorine, bromine, iodine, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, C 1～5 Alkoxy.

[0355] Furthermore, the compound is one of the following compounds:

[0356] The present invention also provides a prodrug of the compound represented by formula XI, or a stereoisomer thereof, or a deuterated derivative thereof, or a salt thereof, or a solvate thereof:

[0357] R1' and R2' are linked to form a 3-10 membered cycloalkyl group substituted by n' R3's, a 3-10 membered heterocycloalkyl group substituted by n' R3's, a 6-10 membered aryl group substituted by n' R3's, or a 5-10 membered heteroaryl group substituted by n' R3's; or R1' and R2' are linked to form

[0358] n' is an integer selected from 0 to 8;

[0359] R3' is selected from C1-C8 alkyl, C1-C8 alkoxy, halogen, hydroxy, nitro, amino, cyano, -C(O)OR5', -C(O)R5';

[0360] R5' is selected from hydrogen, C1-C8 alkyl;

[0361] L'selected

[0362] n1', n2', n3' are independently selected from integers of 0 to 8; and any carbon atom on the main chain of n1', n2', n3' may be replaced by a heteroatom or not; the heteroatom is O, N or S;

[0363] Each R6', R7', R8', R9', R 10 '、R 11 '、R 12 'are independently selected from hydrogen, C1~C8 alkyl;

[0364] Ring A is selected from 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, and 5-10 membered heteroaryl;

[0365] R 13 ' is a substituent on ring A, n4' is R 13 '; n4' is an integer selected from 0 to 8;

[0366] Each R 13 'are independently selected from C1~C8 alkyl, C1~C8 alkoxy, halogen, hydroxy, nitro, amino, cyano;

[0367] R4' is selected from a' R 14 'substituted 3-10 membered cycloalkyl, a' R 14 'substituted 3-10 membered heterocycloalkyl, a' R 14 'substituted 6-10 membered aryl, a' R 14 'Substituted 5- to 10-membered heteroaryl, -C(O)NR d3 R d4 、

[0368] a' is an integer selected from 0 to 8;

[0369] Each R4' is independently selected from C1-C8 alkyl, C1-C8 alkoxy, halogen, hydroxy, nitro, amino, cyano, -C(O)OR 15 '、-C(O)R 15 ', -O(CH2) b’ R 15 ';

[0370] R 15 'Selected from hydrogen, C1~C8 alkyl, C2~C8 alkenyl, C2~C8 alkynyl, (CH2) c’ C(O)R 16 ', by p' R 17 'Substituted 6- to 10-membered aryl;

[0371] b' and c' are independently selected from integers from 0 to 8;

[0372] R 16 ' is selected from hydrogen, C1~C8 alkyl, C2~C8 alkenyl, C2~C8 alkynyl;

[0373] p' is an integer selected from 0 to 8;

[0374] Each R 17 'are independently selected from C1~C8 alkyl, C1~C8 alkoxy, halogen, hydroxy, nitro, amino, cyano;

[0375] R d1 、R d2 、R d3 、R d4 are independently selected from hydrogen, C1-C8 alkyl;

[0376] n1, n, m, R0, R1, R2, R3, R4, R5, R6, R7, R8, R9, R 10 、R 11 As shown in any one of claims 1 to 44.

[0377] The present invention also provides a compound represented by Formula XII, or a stereoisomer thereof, or a deuterated derivative thereof, or a prodrug thereof, or a salt thereof, or a solvate thereof:

[0378] in,

[0379] m is 0 or 1; when m is 0, the connection between R8 and R0 and the connection between R8 and R3 When m is 1, R8 and R0 are connected, and R8 and R3 are connected. is the key;

[0380] Connect R1 and R4 is a key or None;

[0381] Connect R 10 , R5, R2, R7, R 11 of According to the number of bonds connecting carbon atoms, it is bonded or absent;

[0382] R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 、-CR 12 =NR 13 、-CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0383] R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form =NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring;

[0384] L1, L2, L3, L4, and L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0385] R x1 、R x2 、R x3 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x1 、R x2 、R x3The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0386] R3, R 10 Each independently selected from -L6L7L8R x4 ;

[0387] L6, L7, L8 are each independently selected from the following groups: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0388] R x4 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0389] R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , =C(L 12 R X6 )(L 13 R X7 ), =O; or R4 and R5 or R6 and R7 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carboheterocyclic ring;

[0390] L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-, -NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0391] R x5 、R x6 、R x7 Each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x5 、R x6 、R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0392] R8 and R9 are each independently selected from -L 14 L 15 L 16 R X8 ;

[0393] L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkynylidene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-、-CONR 13 -、-CR 12 R 13 NR 14 -; said L 14 , L 15 , L 16 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0394] R x8 A group selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, or the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, -N=NR 12 、-CR 12 =NR 13 ; the R x8 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl;

[0395] R 11 Selected from hydrogen, deuterium, tritium, halogen, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl;

[0396] R 12 、R 13 、R 14 、R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, and 3- to 10-membered heterocycloalkyl.

[0397] The present invention also provides the use of the aforementioned compound, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, or the prodrug of the aforementioned compound represented by formula XI, or its stereoisomer, or its deuterated derivative, or its salt, or its solvate, or the aforementioned compound represented by formula XII, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate in the preparation of a drug for improving respiratory function in inhalation general anesthesia with retained spontaneous breathing.

[0398] Furthermore, the inhalation general anesthesia refers to an anesthesia method induced and maintained by isoflurane, sevoflurane, desflurane, enflurane, enflurane, or nitrous oxide.

[0399] The present invention also provides the use of the aforementioned compound, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, or the prodrug of the aforementioned compound represented by Formula XI, or its stereoisomer, or its deuterated derivative, or its salt, or its solvate, or the compound represented by Formula XII, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate in the preparation of a drug for improving respiratory function in respiratory depression induced by opioid overdose.

[0400] Furthermore, the opioid drug is morphine, fentanyl, sufentanil, remifentanil, alfentanil, carfentanil and other fentanyl derivatives, pethidine, tramadol, dezocine, pentazocine, hydromorphone, oxycodone, buprenorphine, butorphanol, and nalbuphine.

[0401] The present invention also provides an anesthetic and / or sedative antagonist, which is a preparation prepared by using the aforementioned compound, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, or the prodrug of the compound represented by the aforementioned formula XI, or its stereoisomer, or its deuterated derivative, or its salt, or its solvate, or the compound represented by the aforementioned formula XII, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate as the active ingredient, and adding pharmaceutically acceptable excipients.

[0402] Furthermore, the preparation is a tablet, capsule, oral liquid, granule, pill, powder, injection or powder injection.

[0403] The compounds and derivatives provided herein can be named according to the IUPAC (International Union of Pure and Applied Chemistry) or CAS (Chemical Abstracts Service, Columbus, OH) nomenclature system.

[0404] Definitions of terms used in the present invention: Unless otherwise stated, the initial definitions provided for groups or terms in this document apply to the groups or terms throughout the specification; for terms that are not specifically defined herein, they should be given the meaning that a person skilled in the art would give them based on the disclosure and context.

[0405] "Substitution" refers to the replacement of a hydrogen atom in a molecule by another different atom or molecule.

[0406] The minimum and maximum carbon atom content in a hydrocarbon group is indicated by a prefix, for example, the prefix C a ~C b Alkyl refers to any alkyl group containing from "a" to "b" carbon atoms. Thus, for example, "C1-C8 alkyl" refers to an alkyl group containing from 1 to 8 carbon atoms; and "C1-C8 alkoxy" refers to an alkoxy group containing from 1 to 8 carbon atoms.

[0407] "Alkyl" refers to a saturated hydrocarbon chain having a specified number of carbon atoms. For example, C1-C8 alkyl refers to an alkyl group having from 1 to 8 carbon atoms, i.e., 1, 2, 3, 4, 5, 6, 7, or 8 carbon atoms. Alkyl groups can be straight or branched. Representative branched alkyl groups have one, two, or three branches. Alkyl groups include methyl, ethyl, propyl (n-propyl and isopropyl), butyl (n-butyl, isobutyl, and tert-butyl), pentyl (n-pentyl, isopentyl, and neopentyl), and hexyl, heptyl, octyl, and the like.

[0408] "Alkenyl" refers to an unsaturated hydrocarbon chain with at least one carbon-carbon double bond. For example, C2-8 alkenyl refers to an alkenyl group having 2 to 8 carbon atoms, i.e., 2, 3, 4, 5, 6, 7 or 8 carbon atoms. Alkenyl groups can be straight or branched. wait.

[0409] "Alkynyl" refers to an unsaturated hydrocarbon chain with at least one carbon-carbon triple bond. For example, C2-8 alkynyl refers to an alkenyl group having 2 to 8 carbon atoms, i.e., 2, 3, 4, 5, 6, 7 or 8 carbon atoms. Alkenyl groups can be straight or branched. wait.

[0410] "Halogen" is fluorine, chlorine, bromine or iodine.

[0411] "Cycloalkyl" refers to a saturated or unsaturated all-carbon monocyclic or polycyclic ring (including fused, spiro or bridged rings) without a conjugated π electron system, including but not limited to:

[0412] "Heterocycloalkyl" refers to a cycloalkyl group in which at least one carbon atom is replaced by a heteroatom, wherein the heteroatom is O, N or S, and is a saturated or unsaturated monocyclic or polycyclic ring (including fused rings, spiro rings or bridged rings) without a conjugated π electron system, including but not limited to: Oxirane, aziridine, azetidinyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, pyrrolidinyl, piperidinyl,

[0413] "Aryl" refers to an all-carbon monocyclic or polycyclic ring (including fused, spiro or bridged rings) with a conjugated π electron system, including but not limited to phenyl, naphthyl, phenanthrenyl, anthracenyl, fluorenyl and indenyl. The aromatic ring may be fused to other cyclic groups (including saturated and unsaturated rings), but cannot contain heteroatoms such as O, N or S. At the same time, the point of attachment to the parent group must be on a carbon atom on the ring with a conjugated π electron system, including but not limited to

[0414] "Heteroaryl" refers to an aromatic group in which at least one carbon atom of the conjugated π-electron system is replaced by a heteroatom, such as O, N or S, including but not limited to:

[0415] In the present invention, -L a L b L cR d -L a L b L c The structure of - is -L a -L b -L c -, including but not limited to:

[0416] The present invention provides the use of a cyclic ketone compound represented by formula I and a prodrug thereof in the preparation of a drug for improving respiratory depression caused by anesthetics and / or sedatives. The present invention discovers for the first time that the cyclic ketone compound and its prodrug can significantly improve respiratory depression caused by anesthetics and / or sedatives. Experimental results show that the compound of the present invention and its prodrug can improve respiratory function in inhaled general anesthesia with retained spontaneous breathing; at the same time, compared with sodium camphorsulfonate and oxidized camphor, the compound of the present invention can significantly improve respiratory depression induced by opioids at a lower dose, and the minimum dose that induces adverse reactions is higher, and the safety is better. The present invention has a good improvement effect on respiratory depression caused by opioids and inhaled anesthetics, provides a new solution for respiratory depression caused by clinical anesthesia, and has broad application prospects.

[0417] Obviously, based on the above contents of the present invention, according to common technical knowledge and customary means in this field, without departing from the above basic technical ideas of the present invention, other various forms of modifications, replacements or changes can be made.

[0418] The following further describes the above content of the present invention in detail through specific embodiments in the form of examples. However, this should not be construed as limiting the scope of the above subject matter of the present invention to the following examples. All technologies implemented based on the above content of the present invention fall within the scope of the present invention. DETAILED DESCRIPTION

[0419] The raw materials and equipment used in the specific embodiments of the present invention are all known products and are obtained by purchasing commercial products.

[0420] Example 1. Preparation of Compounds

[0421] a1) Preparation of representative compound 45

[0422] Compound 45-1 (1.00 g, 6.02 mmol) was dissolved in 25 mL of tetrahydrofuran under nitrogen. After cooling to -78°C in the cold trap, the mixture was stirred and cooled for 20 minutes. Then, 45-2 (1.37 g, 7.22 mmol) was added dropwise and allowed to react at -78°C for 4 h. TLC monitoring (PE:EA = 10:1, v / v, Rf = 0.2) was performed. After completion, the reaction was terminated by adding 10 mL of hydrochloric acid in dioxane. The tetrahydrofuran solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and the sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA=30:1, v / v, to obtain 0.52 g of target intermediate 45-3, with a yield of 51.38%. ESI-MS: 337.20 (2M+H) + . 1 H NMR(500MHz,Chloroform-d)δ4.25(dd,J=6.6,2.7Hz,1H),3.65(d,J=2.7Hz,1H) ,2.11(dddt,J=6.8,5.3,3.8,1.5Hz,1H),1.82(ddd,J=12.2,7.7,5.7Hz,1H),1.7 0(ddt,J=12.1,7.5,5.3Hz,1H),1.60(ddd,J=12.1,7.6,5.7Hz,1H),1.48(ddt,J= 11.9,7.5,5.3Hz,1H),1.09(s,2H),0.99(d,J=1.4Hz,3H),0.94(d,J=1.4Hz,3H).

[0423] Compound 45-3 (0.52 g, 3.09 mmol) was dissolved in 25 mL of dichloromethane. After cooling to -10°C, the mixture was placed in the cold trap with stirring and cooled for 20 minutes. Then, 45-4 (0.5734 g, 3.71 mmol) and 45-5 (0.9383 g, 9.27 mmol) were added dropwise. The mixture was then transferred from -10°C to 0°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the dichloromethane solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (3 times 100 mL). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.45 g of target compound 45, with a yield of 50.84%. ESI-MS: 287.13 (M+1) + .1 H NMR(500MHz,Chloroform-d)δ7.33–7.21(m,5H),5.49(d,J=6.2Hz,1H),3.73–3.62(m,2H),2.42(tdq,J=7.2,4.6,1.5Hz,1H),1.87–1.71( m,2H),1.62(ddd,J=11.7,7.0,5.6Hz,1H),1.55(ddt,J=12.1,7.3,5.5Hz,1H),1.08(s,2H),1.00(d,J=1.4Hz,3H),0.95(d,J=1.6Hz,3H).

[0424] a2) Preparation of representative compound 40

[0425] The preparation process of compound 45-3 is the same as the first step of the preparation of compound 45.

[0426] Compound 45-3 (0.50 g, 2.97 mmol) was dissolved in 25 mL of dichloromethane. After cooling to -10°C in a cold trap, the mixture was stirred and cooled for 20 minutes. Compounds 40-1 (0.4729 g, 3.57 mmol) and 45-5 (0.9022 g, 8.92 mmol) were then added dropwise. The mixture was then transferred from -10°C to 0°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the dichloromethane solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (3 times 100 mL). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA=50:1, v / v, to obtain 0.37 g of target compound 40, with a yield of 47.09%. ESI-MS: 265.17 (M+1) + . 1 H NMR(500MHz,Chloroform-d)δ5.50(d,J=5.9Hz,1H),2.49–2.38(m,3H),2.01–1.91(m,2H),1.87–1.80(m,1H),1.83–1.77(m,1H),1.80–1.76 (m,1H),1.75(ddd,J=12.6,6.2,4.8Hz,2H),1.71–1.55(m,7H),1.57–1.50(m,1H),1.08(s,3H),1.00(d,J=1.4Hz,4H),0.95(d,J=1.6Hz,4H).

[0427] a3) Preparation of Representative Compound 48

[0428] The preparation process of compound 45-3 is the same as the first step of the preparation of compound 45.

[0429] Compound 45-3 (0.52 g, 3.09 mmol) was dissolved in 25 mL of DMF, followed by the addition of 48-2 (1.04 g, 9.27 mmol). The mixture was stirred at room temperature for 20 minutes, followed by the addition of 48-1 (0.4487 g, 3.71 mmol), and the reaction was carried out at 50°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.29 g of the target compound 48 in a 45.04% yield. ESI-MS: 209.14 (M+1). + . 1 H NMR(500MHz,Chloroform-d)δ4.42(d,J=6.0Hz,1H),3.68(p,J=4.7Hz,1H),2.15(dddt,J= 7.0,5.5,4.2,1.6Hz,1H),1.82(ddd,J=12.0,7.5,5.5Hz,1H),1.74(ddt,J=12.1,7.3,5.4 Hz,1H),1.63(ddd,J=12.0,7.3,5.5Hz,1H),1.59–1.51(m,2H),1.54–1.46(m,1H),1.45–1 .37(m,1H),1.40–1.33(m,1H),1.07(s,2H),0.99(d,J=1.4Hz,3H),0.94(d,J=1.4Hz,3H).

[0430] a4) Preparation of Representative Compound 52

[0431] The preparation process of compound 45-3 is the same as the first step of the preparation of compound 45.

[0432] Compound 45-3 (0.52 g, 3.09 mmol) was dissolved in 25 mL of DMF, followed by the addition of 48-2 (1.04 g, 9.27 mmol). The mixture was stirred at room temperature for 20 minutes, followed by the addition of 52-1 (0.4635 g, 3.71 mmol), and the reaction was carried out at 50°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.31 g of the target compound 52 in a 47.24% yield. ESI-MS: 213.14 (M+1). + . 1 H NMR(500MHz,Chloroform-d)δ4.57–4.52(m,3H),3.32(s,2H),2.23(dddt,J=7.2,5.7,4.3,1.6Hz,1H),1.82(ddd,J=12.0,7.5,5.5Hz,1H),1.79 –1.70(m,1H),1.61(ddd,J=12.0,7.3,5.5Hz,1H),1.47(ddt,J=12.1,7.5,5.5Hz,1H),1.07(s,2H),0.99(d,J=1.4Hz,3H),0.94(d,J=1.4Hz,3H).

[0433] a5) Preparation of Representative Compound 59

[0434] The preparation process of compound 45-3 is the same as the first step of the preparation of compound 45.

[0435] Compound 45-3 (0.52 g, 3.09 mmol) was dissolved in 25 mL of DMF, followed by the addition of 48-2 (1.04 g, 9.27 mmol). The mixture was stirred at room temperature for 20 minutes, followed by the addition of 59-1 (0.7458 g, 3.71 mmol), and the reaction was carried out at 50°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.34 g of the target compound 59 in a 38.14% yield. ESI-MS: 289.17 (M+1).+ . 1 H NMR(500MHz,Chloroform-d)δ7.21(dt,J=8.3,1.0Hz,2H),6.93–6.87(m,2H),4.59(t,J= 1.0Hz,2H),4.48(d,J=5.5Hz,1H),3.78(s,2H),2.22(qdd,J=5.5,2.9,1.5Hz,1H),1.82(d dd,J=12.0,7.5,5.5Hz,1H),1.79–1.70(m,1H),1.63(ddd,J=12.1,7.2,5.5Hz,1H),1.48 (ddt,J=12.1,7.3,5.5Hz,1H),1.07(s,2H),0.99(d,J=1.4Hz,3H),0.94(d,J=1.4Hz,3H).

[0436] a6) Preparation of Representative Compound 62

[0437] The preparation process of compound 45-3 is the same as the first step of the preparation of compound 45.

[0438] Compound 45-3 (0.52 g, 3.09 mmol) was dissolved in 25 mL of dichloromethane. After cooling to -10°C in a cold trap, the mixture was stirred and cooled for 20 minutes. Compounds 62-1 (0.4769 g, 3.71 mmol) and 45-5 (0.9383 g, 9.27 mmol) were then added dropwise. The mixture was then transferred from -10°C to 0°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the dichloromethane solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (3 times 100 mL). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA=50:1, v / v, yielding 0.36 g of target compound 62, with a yield of 44.74%. ESI-MS: 261.10 (M+1) + . 1H NMR(500MHz,Chloroform-d)δ5.06(d,J=7.1Hz,1H),3.23(q,J=9.4Hz,2H),2.30(tdt,J=6.8,3.9,1.6Hz,1H),1.81(ddd,J=12.1,7.5,5.3Hz, 1H),1.75–1.59(m,2H),1.48(ddt,J=11.7,7.1,5.3Hz,1H),1.34(t,J=9.4Hz,3H),1.06(s,2H),0.99(d,J=1.4Hz,3H),0.94(d,J=1.6Hz,3H).

[0439] a7) Preparation of Representative Compound 65

[0440] The preparation process of compound 45-3 is the same as the first step of the preparation of compound 45.

[0441] Compound 45-3 (0.52 g, 3.09 mmol) was dissolved in 25 mL of dichloromethane. After cooling to -10°C in a cold trap, the mixture was stirred and cooled for 20 minutes. Then, 65-1 (0.6551 g, 3.71 mmol) and 45-5 (0.9383 g, 9.27 mmol) were added dropwise. The mixture was then transferred from -10°C to 0°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the dichloromethane solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (3 times 100 mL). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA=50:1, v / v, yielding 0.36 g of target compound 65, with a yield of 37.77%. ESI-MS: 309.10 (M+1) + . 1 H NMR(500MHz,Chloroform-d)δ7.73–7.58(m,5H),5.09(d,J=7.0Hz,1H),2.33(dddt,J=6.8,5.3,3.9,1.5Hz,1H),1.81(ddd,J=12.1 ,7.5,5.3Hz,1H),1.75–1.59(m,2H),1.48(ddt,J=11.5,7.0,5.3Hz,1H),1.06(s,2H),0.99(d,J=1.4Hz,3H),0.94(d,J=1.6Hz,3H).

[0442] a8) Preparation of Representative Compound 78

[0443] The preparation process of compound 45-3 is the same as the first step of the preparation of compound 45.

[0444] Compound 45-3 (0.52 g, 3.09 mmol) was dissolved in 25 mL of dichloromethane. After cooling to -10°C, the mixture was placed in the cold trap with stirring for 20 minutes. Compounds 78-1 (0.5214 g, 3.71 mmol) and 45-5 (0.9383 g, 9.27 mmol) were then added dropwise. The mixture was allowed to react at -10°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the dichloromethane solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (3 times 100 mL). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA=50:1, v / v, to obtain 0.52 g of target compound 78-2, with a yield of 61.77%. ESI-MS: 273.14 (M+1) + .

[0445] Compound 78-2 (0.52 g, 1.91 mmol) was dissolved in 25 mL of DMF, followed by the addition of 48-2 (0.6428 g, 5.73 mmol). The mixture was stirred at room temperature for 20 minutes, followed by the addition of 78-3 (0.3252 g, 2.29 mmol), and the reaction was carried out at 50°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.33 g of the target compound 78 in a 60.35% yield. ESI-MS: 287.15 (M+1). + . 1 H NMR(500MHz,Chloroform-d)δ8.07–8.00(m,2H),7.58–7.51(m,1H),7.49–7.41(m,2H),2.52(dddq,J=7.7,4.6,3.1,1.5Hz, 1H),1.84–1.71(m,2H),1.67–1.57(m,2H),1.34(d,J=1.4Hz,3H),1.09(s,2H),1.01(d,J=1.4Hz,3H),0.96(d,J=1.4Hz,3H).

[0446] a9) Preparation of representative compound 86

[0447] The preparation process of compound 45-3 is the same as the first step of the preparation of compound 45.

[0448] Compound 45-3 (0.52 g, 3.09 mmol) was dissolved in 25 mL of dichloromethane. After cooling to -10°C in a cold trap, the mixture was stirred and cooled for 20 minutes. 86-1 (0.5007 g, 3.71 mmol) and 48-2 (0.9383 g, 9.27 mmol) were then added dropwise. The mixture was allowed to react at 50°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the dichloromethane solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (3 times 100 mL). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA=50:1, v / v, to obtain 0.52 g of target compound 86-2, with a yield of 75.67%. ESI-MS: 223.13 (M+1) + .

[0449] Compound 86-2 (0.52 g, 2.34 mmol) was dissolved in 25 mL of DMF, followed by the addition of 48-2 (0.7874 g, 7.02 mmol). The mixture was stirred at room temperature for 20 minutes, followed by the addition of 78-3 (0.3984 g, 2.81 mmol), and the reaction was carried out at 50°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.31 g of the target compound 86 in a 56.08% yield. ESI-MS: 237.17 (M+1). + . 1H NMR(500MHz,Chloroform-d)δ3.52(dd,J=11.2,4.8Hz,1H),3.41(dd,J=11.4,4.8Hz,1H),2.18(tdq,J=6.1,3.1,1.5Hz,1H),1.82–1.60(m,3H) ,1.56(dddd,J=11.7,6.8,5.9,4.9Hz,1H),1.24–1.14(m,4H),1.08(s,2H),1.00(d,J=1.4Hz,3H),0.95(d,J=1.4Hz,3H),0.33(d,J=5.8Hz,4H).

[0450] a10) Preparation of Representative Compound 105

[0451] The preparation process of compound 45-3 is the same as the first step of the preparation of compound 45.

[0452] Compound 45-3 (0.52 g, 3.09 mmol) was dissolved in 25 mL of dichloromethane. After cooling to -10°C, the mixture was placed in the cold trap with stirring for 20 minutes. Compounds 105-1 (0.5214 g, 3.71 mmol) and 45-5 (0.9383 g, 9.27 mmol) were then added dropwise. The mixture was allowed to react at -10°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the dichloromethane solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (3 times 100 mL). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA=50:1, v / v, to obtain 0.50 g of the target compound 105-2, with a yield of 59.39%. ESI-MS: 273.10 (M+1) + .

[0453] Compound 105-2 (0.50 g, 2.25 mmol) was dissolved in 25 mL of DMF, followed by the addition of 48-2 (0.7571 g, 6.75 mmol). The mixture was stirred at room temperature for 20 minutes, followed by the addition of 78-3 (0.3831 g, 2.70 mmol), and the reaction was carried out at 50°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.32 g of the target compound 105 in a 60.20% yield. ESI-MS: 287.12 (M+1). + . 1 H NMR(500MHz,Chloroform-d)δ3.57(p,J=7.5Hz,1H),2.25(tdq,J=6.0,2.9,1.5Hz,1H),1.85–1.59(m,8H),1.53(dd dd,J=11.8,6.8,5.8,4.9Hz,1H),1.34(d,J=1.6Hz,3H),1.08(s,2H),1.01(d,J=1.4Hz,3H),0.96(d,J=1.4Hz,3H).

[0454] b) Preparation of representative compound 02 and its prodrugs 02-prodrug-1 and 02-prodrug-2

[0455] Compound 02-0 (0.50 g, 3.01 mmol) was dissolved in 25 mL of tetrahydrofuran, and 02-2 (79.41 mg, 3.31 mmol) was added. The mixture was stirred at room temperature for 30 minutes, followed by 02-1 (1.28 g, 3.61 mmol). The reaction was heated to 60°C for 8 hours and monitored by TLC (PE:EA = 30:1, v / v, Rf = 0.3). After completion of the reaction, the tetrahydrofuran solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and the sample was then mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 100:1, v / v, yielding 0.14 g of the target compound 02 in a 25.27% yield. ESI-MS:185.14.1H NMR(500MHz,Chloroform-d)δ2.30(dddd,J=24.9,12.3,7.0,5.2Hz,1H),2.20–2.06(m,1H),1.96(ddd ,J=12.4,7.1,5.3Hz,1H),1.82(ddd,J=12.3,7.1,5.2Hz,1H),1.22(s,2H),1.13(s,2H),1.08(s,2H).

[0456] The parent drug 02 (1.00 g, 5.43 mmol) was dissolved in 15 mL of toluene, and 02-3 (463.31 mg, 6.51 mmol) and 02-4 (1.85 g, 6.51 mmol) were added. The reaction was microwaved at 130°C for 2 h and monitored by TLC (DCM:MeOH = 20:1, v / v, Rf = 0.2). The reaction mixture was transferred to an eggplant-shaped flask, and the toluene solvent was evaporated under reduced pressure. 100 mL of saturated sodium chloride solution was added, and the mixture was extracted with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and then purified on a silica gel plate. The developing solvent was DCM:MeOH = 20:1, v / v. The target band was collected to yield 0.72 g of the target compound (compound 02-prodrug-1) in a yield of 45.67%. ESI-MS:291.17.1H NMR(500MHz,Chloroform-d)δ3.72–3.64(m,1H),3.59–3.51(m,1H),2.29–2.06(m,2H),1.94–1.64(m,12H),1.14(d,J=12.8Hz,4H),1.08(s,2H).

[0457] The parent drug 02 (1.00 g, 5.43 mmol) was dissolved in 25 mL of toluene, and 02-5 (587.08 mg, 6.51 mmol) and 02-6 (1.12 g, 6.51 mmol) were added. The mixture was heated to 120°C with a water separator and refluxed for 24 h. TLC monitoring was performed (DCM:MeOH = 20:1, v / v, Rf = 0.2). The toluene solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and then purified on a silica gel plate. The developing solvent was DCM:MeOH = 20:1, v / v. The target band was collected to yield 0.75 g of the target compound (compound 02-prodrug-2) in a 46.0% yield. ESI-MS:283.14.1H NMR(500MHz,Chloroform-d)δ4.03–3.89(m,4H),3.83(d,J=12.5Hz,1H),3.73(d,J=12.5Hz,1H),2.65(ddq,J=7.3,4.4,1.6Hz,1H),1.82 –1.72(m,2H),1.72–1.62(m,1H),1.50–1.40(m,1H),1.32(s,2H),1.27(s,2H),1.08(s,2H),1.03(d,J=1.4Hz,3H),0.98(d,J=1.6Hz,3H).

[0458] c) Preparation of representative compounds 03, (-)-03, (+)-03 and their prodrugs 03-prodrug-1 and 03-prodrug-2

[0459] Compound 03-0 (0.50 g, 3.01 mmol) was dissolved in 25 mL of N,N-dimethylformamide, and 03-2 (675.09 mg, 6.02 mmol) was added. The mixture was stirred at 45°C for 30 minutes, followed by the addition of 03-1 (0.4946 g, 3.61 mmol). The mixture was heated to 45°C for 8 hours and monitored by TLC (PE:EA = 10:1, v / v, Rf = 0.6). After completion of the reaction, the solvent N,N-dimethylformamide was removed as much as possible by rotary evaporation under reduced pressure. 100 mL of saturated sodium chloride solution was then added, and the mixture was extracted with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA=50:1, v / v, to obtain 0.23 g of target compound 03, with a yield of 34.39%. ESI-MS: 223.23. 1 H NMR(500MHz,Chloroform-d)δ1.98(qt,J=7.0,5.3Hz,1H),1.94–1.83(m,2H),1.78–1.69(m,1H),1.63–1.5 4(m,1H),1.31(qd,J=7.3,5.3Hz,2H),1.18(s,2H),1.04(s,2H),1.01–0.92(m,5H),0.89(t,J=7.3Hz,3H).

[0460] Compound 03 (0.50 g, 2.25 mmol) was dissolved in 25 mL of dichloromethane. The chiral reducing agent (+)-B-diisopinocampheylborane ((+)-DIP-Chloride) (1.58 g, 4.72 mmol) was added and stirred at 30°C for 120 minutes. TLC monitoring (PE:EA = 20:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the dichloromethane solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was extracted with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. Filtration and evaporation of the solvent were performed, and the product was recrystallized from an EtOH-H2O mixed solvent system to obtain 0.13 g of the target compound (-)-03 in a 26.00% yield. ESI-MS: 223.24.1H NMR (500 MHz, Chloroform-d) δ 1.99 (qt, J = 7.0, 5.3 Hz, 1H), 1.95–1.85 (m, 2H), 1.74 (ddd, J = 11.7, 6.7, 4.3 Hz, 1H), 1.62–1.54 (m, 1H), 1.31 (qd, J = 7.3, 5.3 Hz, 2H), 1.21 (s, 2H), 1.04 (s, 2H), 1.00 (s, 2H), 0.95 (d, J = 6.9 Hz, 3H), 0.89 (t, J = 7.3 Hz, 3H). The intermediate 03-7 (0.26 g, 1.15 mmol) was recovered and oxidized with Dess-martin (1.07 g, 2.53 mmol) to give the target compound (+)-03. 0.10 g, 39.16% yield. ESI-MS: 223.21. 1H NMR (500 MHz, Chloroform-d) δ 1.99 (qt, J = 6.9, 5.3 Hz, 1H), 1.96–1.83 (m, 2H), 1.73 (ddd, J = 11.9, 5.9, 4.3 Hz, 1H), 1.59 (ddd, J = 12.3, 6.1, 4.3 Hz, 1H), 1.31 (qd, J = 7.3, 5.3 Hz, 2H), 1.21 (s, 2H), 1.04 (s, 2H), 1.00 (s, 2H), 0.95 (d, J = 6.9 Hz, 3H), 0.89 (t, J = 7.3 Hz, 3H).

[0461] The parent drug 03 (1.00 g, 4.50 mmol) was dissolved in 15 mL of toluene, and 03-3 (383.88 mg, 5.40 mmol) and 03-4 (1.53 g, 5.40 mmol) were added. The reaction was microwaved at 130°C for 2 h and monitored by TLC (DCM:MeOH = 20:1, v / v, Rf = 0.2). The reaction solution was transferred to an eggplant-shaped flask, and the toluene solvent was evaporated under reduced pressure. 100 mL of saturated sodium chloride solution was added, and the mixture was extracted with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and then purified on a silica gel plate. The developing solvent was DCM:MeOH = 20:1, v / v. The target band was collected to obtain 0.68 g of the target compound (compound 03-prodrug-1) in a yield of 46.02%. ESI-MS:329.22.1H NMR(500MHz,Chloroform-d)δ3.61–3.51(m,2H),1.96–1.64(m,12H),1.63–1.55(m,1H) ,1.37–1.26(m,2H),1.09(s,2H),1.02(s,2H),0.98–0.92(m,5H),0.89(t,J=7.3Hz,2H).

[0462] The parent drug 03 (1.00 g, 4.80 mmol) was dissolved in 25 mL of toluene, and 03-5 (519.18 mg, 5.76 mmol) and 03-6 (992.01 mg, 5.76 mmol) were added. The mixture was heated to 120°C with a water separator and refluxed for 24 h. TLC monitoring was performed (DCM:MeOH = 20:1, v / v, Rf = 0.2). The toluene solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and then purified on a silica gel plate. The developing solvent was DCM:MeOH = 20:1, v / v. The target band was collected to yield 0.64 g of the target compound (compound 03-prodrug-2) in a 37.82% yield. ESI-MS:353.22.1H NMR(500MHz,Chloroform-d)δ3.84(d,J=12.3Hz,1H),3.79(d,J=17.9Hz,1H),3.73(d,J=12.5Hz ,1H),1.94(hept,J=5.3Hz,1H),1.85–1.69(m,3H),1.58–1.50(m,1H),1.32(s,4H),1.27(s,5H), 1.08(s,2H),1.02(s,2H),0.97(s,2H),0.94(dd,J=5.4,0.6Hz,5H).

[0463] d) Preparation of representative compound 04, deuterated compound 04-D2 and its prodrugs 04-prodrug-1 and 04-prodrug-2

[0464] Compound 04-1 (200 mg, 1.2 mmol) was suspended in water, and 04-2 SelectFluor (469 mg, 1.32 mmol) was added. The mixture was stirred at 70°C under nitrogen for 10 hours. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 4:1, v / v. 0.12 g of target compound 04 was obtained, with a yield of 54.0%. ESI-MS: 185.07. 1H NMR(400MHz,Chloroform-d)δ4.95–4.88(m,1H),4.86–4.78(m,1H),3.07(ddd,J=14.4,8.8, 5.5Hz,1H),2.89–2.76(m,3H),2.54(tddd,J=16.7,11.9,8.1,4.2Hz,1H),1.83–1.57(m,6H).

[0465] 19 F NMR(377MHz,Chloroform-d)δ-153.46,-166.96.

[0466] Compound 04 (200 mg, 1.09 mmol) was placed in a 100 mL eggplant-shaped flask. A catalytic amount of Pd / C was weighed, and 30 mL of deuterated methanol was added. A thick-walled hydrogen storage balloon filled with deuterated 04-2 was attached to the flask. The atmosphere in the flask was replaced with deuterium three times, and the mixture was stirred at 30°C for 8 hours. After completion of the reaction, the mixture was filtered, the residue was washed three times with methanol, and the solvent was evaporated under reduced pressure. 100 mL of saturated sodium chloride solution was then added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and distillation, and the sample was then subjected to silica gel column chromatography. Developing solvent: PE:EA = 4:1, v / v. 0.14 g of the target compound 04-D2 was obtained in a 68.5% yield. ESI-MS: 189.08. 1 H NMR (500MHz, Chloroform-d) δ2.78–2.65(m,3H),2.03(dtdt,J=10.1,8.6,7.2,1.5Hz,1H),1.83(s,1H),0.87(d,J=1.6Hz,4H).

[0467] The parent drug 04 (1.00 g, 5.43 mmol) was dissolved in 15 mL of toluene, and 04-3 (463.31 mg, 6.51 mmol) and 04-4 (1.85 g, 6.51 mmol) were added. The reaction was microwaved at 130°C for 2 h and monitored by TLC (DCM:MeOH = 20:1, v / v, Rf = 0.2). The reaction solution was transferred to an eggplant-shaped flask, and the toluene solvent was evaporated under reduced pressure. 100 mL of saturated sodium chloride solution was added, and the mixture was extracted with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and then purified on a silica gel plate. The developing solvent was DCM:MeOH = 20:1, v / v. The target band was collected to obtain 0.56 g of the target compound (compound 04-prodrug-1) in a yield of 35.52%. ESI-MS:291.12.1H NMR(500MHz,Chloroform-d)δ4.85(tt,J=1.9,1.0Hz,1H),4.78(tq,J=1.8,0.9Hz,1H),3.53(p,J=5.7Hz,2H),2.9 0–2.79(m,1H),2.66(dd,J=12.4,7.8Hz,2H),2.56(dd,J=12.4,8.0Hz,2H),1.91–1.69(m,14H),1.73–1.61(m,4H).

[0468] The parent drug 04 (1.00 g, 5.43 mmol) was dissolved in 25 mL of toluene, and 04-5 (587.08 mg, 6.51 mmol) and 04-6 (1.12 mg, 6.51 mmol) were added. The mixture was heated to 120°C with a water separator and refluxed for 24 h. TLC monitoring was performed (DCM:MeOH = 20:1, v / v, Rf = 0.2). The toluene solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and then purified on a silica gel plate. The developing solvent was DCM:MeOH = 20:1, v / v. The target band was collected to yield 0.58 g of the target compound (compound 04-prodrug-2) in a 32.53% yield. ESI-MS:329.12.1H NMR(500MHz,Chloroform-d)δ4.80(dq,J=13.1,1.7Hz,4H),3.80(d,J=12.3Hz,3H),3.70(d,J=12.5Hz,3H),2.97(d tdd,J=8.6,7.0,5.3,1.7Hz,2H),2.10–2.00(m,8H),1.75(q,J=1.5Hz,6H),1.64(s,2H),1.32(s,9H),1.27(s,9H).

[0469] e) Preparation of representative compound 05

[0470] Step 1: Compound 05-1 (8.7 g, 120.6 mmol) was dissolved in acetone (20 mL) and water (20 mL) and stirred at 65°C for 3 hours. After completion of the reaction, the pH was adjusted to 2-3 with 1% NaOH solution, and the mixture was extracted with methyl tert-butyl ether. The organic phase was collected, dried, and concentrated to afford intermediate 05-2 (10.0 g, 59%) as a light yellow oil.

[0471] 1 H NMR(400MHz,Chloroform-d)δ6.77(dd,J=16.0,6.7Hz,1H),6.03(dd,J=16.0,1. 4Hz, 1H), 2.47 (dpd, J=13.5, 6.8, 1.5Hz, 1H), 2.25 (s, 3H), 1.08 (d, J=6.8Hz, 6H).

[0472] Step 2: Compound 05-2 (5.0 g, 35.7 mmol) and diethyl malonate were dissolved in ethanol (50 mL), and 20% sodium ethoxide (19.7 g) was added dropwise at room temperature. The reaction solution was stirred at room temperature for 3 hours, then heated to 80°C and refluxed for 2 hours. After the reaction was completed, the reaction solution was concentrated to obtain a residue, which was dissolved in water and washed with ethyl acetate. The aqueous phase was then collected and the pH was adjusted to 4-5 with 10% citric acid. The aqueous phase was then extracted with dichloromethane. The organic phase was collected, dried, and concentrated to obtain the crude product of intermediate 05-3, which was directly used in the next step without further treatment.

[0473] Step 3: The crude product of Intermediate 05-3 was dissolved in ethanol (30 mL) and aqueous sodium hydroxide solution (12 M, 50 mL) was added dropwise at room temperature. The mixture was then allowed to react at room temperature for two days. After completion of the reaction, the mixture was concentrated in vacuo, and the residue was acidified with 10% citric acid. The aqueous phase was then extracted with ethyl acetate, and the organic phase was collected, dried, and concentrated to give the crude product. After purification by column chromatography (30% EA), Intermediate 05-4 (4.87 g) was obtained as a brown oil.

[0474] 1 H NMR (400MHz, Methanol-d4) δ2.43–2.33(m,2H),2.23–2.11(m,2H),1.93–1.78(m,1H),1.69–1.53(m,J=6.7Hz,1H),0.96(d,J=6.8Hz,6H).

[0475] Step 4: Compound 05-4 (1.00 g, 6.48 mmol) was suspended in 5 M NaOH (1.30 mL, 6.48 mmol). Iodomethane (1.84 g, 12.97 mmol) was slowly added dropwise under an ice bath. The mixture was stirred at 65°C under a nitrogen atmosphere for 24 h. The reaction mixture was quenched with 1 M HCl (10 mL) and extracted with ethyl acetate. The organic phase was collected, dried, and concentrated. The residue was separated by column chromatography (PE:EA = 3:1) to afford 05-5 as a white solid in a 65% yield.

[0476] 1 H NMR (400MHz, Methanol-d4) δ2.44 (dd, J=16.6, 4.4Hz, 2H), 2.20 (s, 2H), 1.79 (tdt, J= 11.7, 6.7, 4.4Hz, 1H), 1.63 (s, 3H), 1.56 (hept, J = 6.7Hz, 1H), 0.94 (d, J = 6.7Hz, 6H).

[0477] Step 5: Compound 05-5 (200 mg, 1.19 mmol) was suspended in water, and SelectFluor (463.26 mg, 1.31 mmol) was added. The mixture was stirred at 70°C under nitrogen for 10 hours. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography using a developing solvent of PE:EA = 4:1, v / v, to obtain the target compound 05. The product was 45 mg of a colorless oil with a yield of 20.33%. ESI-MS: 187.08.

[0478] 1H NMR (400MHz, Methanol-d4) δ2.81–2.51(m,4H),1.74(d,J=21.0Hz,4H),1.58(d,J=22.8Hz,1H),0.97(d,J=6.4Hz,6H).

[0479] 19 F NMR(377MHz,Methanol-d4)δ-172.08

[0480] f) Preparation of representative compound 06

[0481] Compound 06-1 (200 mg, 1.2 mmol) was suspended in water, and 06-2 SelectFluor (469 mg, 1.32 mmol) was added. The mixture was stirred at 60°C under nitrogen for 8 hours. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 4:1, v / v, yielded 0.068 g of target compound 06, with a yield of 30.68%. ESI-MS: 185.07. 1 H NMR(400MHz,Chloroform-d)δ2.99–2.82(m,4H),1.64(d,J=22.3Hz,3H),1.20(t d,J=8.3,7.8,4.2Hz,1H),0.56(tdt,J=10.9,6.2,4.0Hz,3H),0.22–0.11(m,2H).

[0482] g) Preparation of representative compound 07

[0483] Compound 07-1 (1.00 g, 7.13 mmol) was suspended in 5M NaOH 07-3 (1.43 mL, 7.13 mmol). Iodomethane 07-2 (2.03 g, 14.27 mmol) was slowly added dropwise under an ice bath. The mixture was stirred at 65°C for 24 h under a nitrogen atmosphere and monitored by TLC (PE:EA=3:1, v / v, Rf=0.2). After completion, the mixture was quenched with 1M HCl (10 mL), and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of ethyl acetate (100 mL×3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and the residue was separated by column chromatography (PE:EA=3:1) to obtain intermediate 07-4 as a white solid compound (650 mg, 59%). ESI-MS: 309.14 (2M+H) + . 1 H NMR (400MHz, Chloroform-d) δ3.41 (qt, J=6.6, 1.1Hz, 1H), 2.33 (d, J=1.1Hz, 4H), 1.20 (s, 2H), 1.07 (s, 6H), 0.81 (s, 3H).

[0484] Compound 07-4 (100 mg, 0.65 mmol) was suspended in water (3 mL) and SelectFluor was added. The compound was then stirred at 70°C for 10 hours under nitrogen. After the reaction was complete, the reaction solution was extracted with ethyl acetate. The organic phase was collected, dried, and concentrated. The resulting residue was separated by column chromatography (PE:EA = 4:1) to obtain the product, Compound 07 (40 mg, 35%), as a white solid. ESI-MS: 345.14 (2M+H) + . 1 H NMR (400MHz, Chloroform-d) δ2.70 (d, J = 3.9 Hz, 4H), 1.68 (d, J = 21.7 Hz, 3H), 1.13 (s, 3H), 0.98 (s, 3H).

[0485] h) Preparation of representative compound 08 and its prodrugs 08-prodrug-1 and 08-prodrug-2

[0486] Compound 08-1 (0.50 g, 3.28 mmol) was dissolved in 25 mL of tetrahydrofuran, and 08-3 (236.82 mg, 3.28 mmol) was added. The mixture was stirred at room temperature for 30 minutes, followed by 08-2 (1.40 g, 3.94 mmol). The reaction was heated to 60°C for 8 hours and monitored by TLC (PE:EA = 30:1, v / v, Rf = 0.3). After completion of the reaction, the tetrahydrofuran solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was then subjected to silica gel column chromatography using PE:EA = 100:1, v / v as the eluent. 0.21 g of the target compound 08 was obtained in a 37.56% yield. ESI-MS: 341.16 (2M+H) + . 1 H NMR(500MHz,Chloroform-d)δ2.74(dddt,J=25.1,5.3,3.9,1.6Hz,1H),2.66(d,J=12.3Hz,1H),2.43(d,J=12.3Hz,1H),1.90(dd,J=12.4 ,3.9Hz,1H),1.79(dd,J=12.5,3.8Hz,1H),1.73(d,J=1.5Hz,2H),1.68(d,J=1.7Hz,2H),1.57–1.50(m,1H),0.92(dd,J=5.1,0.7Hz,7H).

[0487] The parent drug 08 (1.00 g, 5.87 mmol) was dissolved in 15 mL of toluene, and 08-4 (501.37 mg, 7.05 mmol) and 08-5 (2.00 g, 7.05 mmol) were added. The reaction was microwaved at 130°C for 2 h and monitored by TLC (DCM:MeOH = 20:1, v / v, Rf = 0.2). The reaction solution was transferred to an eggplant-shaped flask, and the toluene solvent was evaporated under reduced pressure. 100 mL of saturated sodium chloride solution was added, and the mixture was extracted with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and then purified on a silica gel plate. The developing solvent was DCM:MeOH = 20:1, v / v. The target band was collected to obtain 0.61 g of the target compound (compound 08-prodrug-1) in a yield of 46.49%. ESI-MS:224.13.1H NMR(500MHz,Chloroform-d)δ3.52(p,J=5.8Hz,1H),2.84(dtd,J=25.1,3.5,1.6Hz,1H),2.65(d,J=12.4Hz,1H),2.57 (d,J=12.3Hz,1H),1.94(dd,J=12.5,3.5Hz,1H),1.93–1.62(m,11H),1.55(dt,J=10.0,5.0Hz,1H),0.95–0.90(m,6H).

[0488] The parent drug 08 (1.00 g, 5.87 mmol) was dissolved in 25 mL of toluene, and 08-6 (635.31 mg, 7.05 mmol) and 08-7 (1.21 g, 7.05 mmol) were added. The mixture was heated to 120°C with a water separator and refluxed for 24 h. TLC monitoring was performed (DCM:MeOH = 20:1, v / v, Rf = 0.2). The toluene solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and then purified on a silica gel plate. The developing solvent was DCM:MeOH = 20:1, v / v. The target band was collected to yield 0.56 g of the target compound (compound 08-prodrug-2) in a 39.34% yield. ESI-MS:243.11.1H NMR(500MHz,Chloroform-d)δ3.77(d,J=12.3Hz,1H),3.65(d,J=12.5Hz,1H),2.51(dddd,J=25.1,4.9,3.3,1.5Hz,1H),2.03(d,J=13.0Hz,1H),1.92(d,J =13.0Hz,1H),1.78(dd,J=12.3,3.5Hz,1H),1.73–1.67(m,1H),1.64–1.55(m ,3H),1.52(d,J=1.6Hz,2H),1.32(s,3H),1.27(s,3H),0.91(d,J=4.5Hz,7H).

[0489] i) Preparation of representative compound 09

[0490] Compound 08 (0.30 g, 1.76 mmol) was dissolved in 25 mL of glacial acetic acid, and ground 09-1 (430.25 mg, 3.88 mmol) was added. The mixture was heated to 120°C and refluxed for 24 h. TLC monitoring was performed (PE:EA = 2:1, v / v, Rf = 0.3). After completion of the reaction, the mixture was filtered, and the filter cake was washed twice with glacial acetic acid. The solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and distillation. The sample was mixed and then chromatographed on a silica gel column. The eluent was PE:EA = 10:1, v / v. 0.084 g of the target compound 09 was obtained in a 25.87% yield. ESI-MS: 185.08. 1H NMR(500MHz,Chloroform-d)δ2.84(dddt,J=25.3,5.8,4.4,1.5Hz,1H),2.21–2.13(m,1H), 2.11(dd,J=12.4,4.3Hz,1H),1.84–1.76(m,2H),1.79–1.73(m,2H),0.95(d,J=5.5Hz,6H).

[0491] j1) Preparation of representative compound 1

[0492] Compound 1-1 (0.50 g, 3.01 mmol) was dissolved in 25 mL of methanol, and 1-2 (283.55 mg, 4.51 mmol) was added. The mixture was heated to 60°C for 8 h and monitored by TLC (PE:EA = 20:1, v / v, Rf = 0.3). After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. The eluent was PE:EA = 50:1, v / v. 0.32 g of the target intermediate 1-3 was obtained in a 63.23% yield. ESI-MS: 337.12 (2M+H) + .

[0493] Compound 1-3 (0.32 g, 1.90 mmol) was dissolved in 25 mL of dichloromethane and stirred at -10°C for 10 minutes. Compounds 1-4 (238.60 mg, 2.28 mmol) and 45-5 (0.5774 g, 5.71 mmol) were then added dropwise. The reaction mixture was transferred to 0°C and allowed to react for 8 hours. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.2) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was then mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.16 g of the target compound 1 in a 35.60% yield. ESI-MS: 237.12 (M+H) + . 1H NMR(500MHz,Chloroform-d)δ4.28(d,J=11.7Hz,1H),4.23(d,J=11.7Hz,1H),2.31(dd,J=12.4,5.4Hz,1H),2.23(dd,J=12.4,5.4Hz,1 H),2.15–2.08(m,1H),1.93(p,J=6.5Hz,1H),1.79–1.66(m,2H),1.60–1.49(m,2H),1.14–0.97(m,3H),1.02(s,4H),1.00–0.89(m,2H).

[0494] j2) Preparation of representative compound 5

[0495] The preparation of compound 1-3 is the same as that of compound 1.

[0496] Compound 1-3 (0.32 g, 1.90 mmol) was dissolved in 25 mL of dichloromethane and stirred at -10°C for 10 minutes. Then, 5-1 (399.46 mg, 2.28 mmol) and 45-5 (0.5774 g, 5.71 mmol) were added dropwise. The reaction mixture was transferred to 0°C and allowed to react for 8 hours. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.2) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v) afforded 0.17 g of the target compound 5 in a yield of 29.13%. ESI-MS:307.10(M+H) + . 1 H NMR (500MHz, Chloroform-d) δ7.95–7.89(m,2H),7.46–7.40(m,2H),4.46(d,J=1.4Hz,2H),2.31(dd,J=12.5,5.5Hz,1H),2.24(dd,J =12.5,5.3Hz,1H),2.12(tddd,J=6.9,5.4,3.5,2.0Hz,1H),1.80–1.67(m,2H),1.60–1.49(m,2H),1.06–1.00(m,5H).

[0497] j3) Preparation of representative compound 11

[0498] The preparation of compound 1-3 is the same as that of compound 1.

[0499] Compound 1-3 (0.32 g, 1.90 mmol) was dissolved in 25 mL of DMF, followed by the addition of 48-2 (0.6403 g, 5.71 mmol). The mixture was stirred at room temperature for 20 minutes, followed by the addition of 11-1 (0.3722 g, 2.28 mmol), and the reaction was carried out at 50°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.15 g of the target compound 11, with a yield of 31.50%. ESI-MS: 251.19 (M+1). + . 1 H NMR(500MHz,Chloroform-d)δ3.50(d,J=1.8Hz,2H),3.38(dd,J=11.1,3.6Hz,1H),3.28(dd,J=11.2,3.5Hz,1H),2.32(dd,J=12.5,5. 5Hz,1H),2.23(dd,J=12.5,5.3Hz,1H),2.15–2.06(m,1H),1.81–1.64(m,5H),1.68–1.43(m,6H),1.00(s,2H),0.92(d,J=1.5Hz,3H).

[0500] j4) Preparation of representative compound 16

[0501] The preparation of compound 1-3 is the same as that of compound 1.

[0502] Compound 1-3 (0.32 g, 1.90 mmol) was dissolved in 25 mL of DMF, followed by the addition of 48-2 (0.6403 g, 5.71 mmol). The mixture was stirred at room temperature for 20 minutes, followed by the addition of 16-1 (0.4589 g, 2.28 mmol) and allowed to react at 50°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The combined organic phases were washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.16 g of the target compound 16 in a 29.17% yield. ESI-MS: 289.17 (M+1). + .1 H NMR(500MHz,Chloroform-d)δ7.22(dt,J=8.3,0.9Hz,2H),6.93–6.87(m,2H), 4.53(t,J=1.0Hz,2H),3.78(s,2H),3.59(d,J=1.1Hz,2H),2.32(dd,J=12.5,5 .5Hz,1H),2.23(dd,J=12.5,5.3Hz,1H),2.11(dddd,J=6.8,5.3,3.2,1.5Hz,1 H),1.78–1.68(m,2H),1.65–1.48(m,2H),1.00(s,2H),0.94(d,J=1.4Hz,3H).

[0503] j5) Preparation of representative compound 18

[0504] The preparation of compound 1-3 is the same as that of compound 1.

[0505] Compound 1-3 (0.32 g, 1.90 mmol) was dissolved in 25 mL of dichloromethane and stirred at -10°C for 10 minutes. Compounds 18-1 (261.45 mg, 2.28 mmol) and 45-5 (0.5774 g, 5.71 mmol) were then added dropwise. The reaction mixture was transferred to 0°C and allowed to react for 8 hours. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.2) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.20 g of the target compound 18 in a 42.59% yield. ESI-MS: 247.09 (M+H) + . 1 H NMR(500MHz,Chloroform-d)δ4.06(d,J=12.3Hz,1H),3.84(d,J=12.5Hz,1H),3.11(s,2H),2.31(dd,J=12.5,5.5Hz,1H),2 .25(dd,J=12.5,5.3Hz,1H),2.15–2.07(m,1H),1.80–1.68(m,2H),1.60–1.48(m,2H),1.02(s,2H),0.97(d,J=1.4Hz,3H).

[0506] j6) Preparation of representative compound 23

[0507] The preparation of compound 1-3 is the same as that of compound 1.

[0508] Compound 1-3 (0.32 g, 1.90 mmol) was dissolved in 25 mL of dichloromethane and stirred at -10°C for 10 minutes. Compound 23-1 (481.74 mg, 2.28 mmol) and compound 45-5 (0.5774 g, 5.71 mmol) were then added dropwise. The mixture was transferred to 0°C and allowed to react for 8 hours. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.2) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.17 g of the target compound 23 in a 26.07% yield. ESI-MS:343.06(M+H) + . 1 H NMR(500MHz,Chloroform-d)δ7.85–7.79(m,2H),7.55–7.49(m,2H),3.90(d,J=12.5Hz,1H),3.57(d,J=12.3Hz,1H),2.31(dd,J=12.5,5.5Hz,1H) ,2.25(dd,J=12.5,5.3Hz,1H),2.11(ttd,J=5.3,4.4,3.8,1.4Hz,1H),1 .80–1.68(m,2H),1.60–1.48(m,2H),1.02(s,2H),0.97(d,J=1.4Hz,3H).

[0509] j7) Preparation of representative compound 30

[0510] Compound 1-1 (0.50 g, 3.01 mmol) was dissolved in 25 mL of tetrahydrofuran (THF) and stirred at -78°C for 10 minutes. Then, 30-1 (970.55 mg, 6.02 mmol) was added dropwise. The mixture was transferred to 0°C and allowed to react for 8 hours. TLC monitoring (PE:EA = 20:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and the sample was then purified by silica gel column chromatography using PE:EA = 50:1, v / v as the eluent. The target compound 30 (0.26 g) was obtained in a 38.53% yield. ESI-MS: 225.17 (M+H)+ . 1 H NMR(500MHz,Chloroform-d)δ3.70–3.61(m,1H),2.49(d,J=5.5Hz,1H),2.33(dd,J=12.3,5.5Hz,1H),2.28(dd,J=12.5,5.3Hz,1H),2.12–2.04(m,1H), 1.81–1.63(m,3H),1.66–1.37(m,4H),1.03–0.95(m,5H),0.89(dd,J=6.2,0.7Hz,6H).

[0511] j8) Preparation of representative compound 37

[0512] Compound 1-1 (0.32 g, 1.93 mmol) was dissolved in 25 mL of tetrahydrofuran (THF) and stirred at -78°C for 10 minutes. Then, 37-1 (752.13 mg, 3.85 mmol) was added dropwise. The mixture was transferred to 0°C and allowed to react for 8 hours. TLC monitoring (PE:EA = 20:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and the sample was then purified by silica gel column chromatography using PE:EA = 50:1, v / v as the eluent. The target compound 37 (0.19 g) was obtained in a 38.20% yield. ESI-MS: 259.16 (M+H) + . 1 H NMR(500MHz,Chloroform-d)δ7.20–7.14(m,2H),7.14–7.09(m,2H),4.77(dtd,J=5.7,2.5,1 .3Hz,1H),3.43(d,J=5.9Hz,1H),2.34(s,2H),2.32–2.22(m,2H),2.11(tdt,J=6.5,5.2,3.0H z,1H),1.84(ddd,J=12.1,7.7,5.8Hz,1H),1.73(dddd,J=12.2,7.7,5.8,4.7Hz,1H),1.61(d dd,J=12.1,7.4,5.7Hz,1H),1.52(dddd,J=12.3,7.7,5.9,4.7Hz,1H),1.06(d,J=1.3Hz,6H).

[0513] k1) Preparation of representative compound 119

[0514] Compound 119-1 (1.00 g, 5.10 mmol) was dissolved in 25 mL of dichloromethane, and HATU (2.91 g, 7.64 mmol) was added. The mixture was stirred at -10°C for 30 minutes, followed by the addition of 119-2 (447.23 mg, 6.11 mmol) and DIPEA (1.98 g, 15.29 mmol). The reaction was transferred to 40°C and allowed to react for 8 hours. TLC monitoring (PE:EA = 20:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was evaporated, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA=50:1, v / v, yielded target intermediate 119-30.82 g, yield 64.02%. ESI-MS: 252.32 (M+H) + .

[0515] Compound 119-3 (0.82 g, 3.26 mmol) was dissolved in 25 mL of toluene, and 119-4 (242.97 mg, 3.91 mmol) was added. A water separator was installed and the reaction was refluxed at 120°C for 6 hours. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and the sample was mixed. The product was then purified by silica gel column chromatography using the developing solvent: PE:EA = 50:1, v / v. 0.62 g of the target intermediate 119-5 was obtained in a yield of 64.33%. ESI-MS: 296.20 (M+H) + .

[0516] Compound 119-5 (0.62 g, 2.10 mmol) was dissolved in 25 mL of toluene, and 119-6 (506.59 mg, 2.52 mmol) was added. The reaction was continued at 60°C for 8 hours, monitored by TLC (PE:EA = 5:1, v / v, Rf = 0.3). After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, the sample was mixed, and the mixture was purified by silica gel column chromatography. Developing solvent: PE:EA = 10:1, v / v, yielding 0.31 g of the target compound 119-8 in a 52.48% yield. ESI-MS: 282.20 (M+H) + .

[0517] Compound 119-8 (0.31 g, 1.10 mmol) was dissolved in 25 mL of ethyl acetate, and a solution of HCl in 1,4-dioxane (dioxane hydrocholoride) 119-7 was added. The reaction was allowed to proceed at 40°C for 8 hours. After completion of the reaction, the solvent was evaporated under reduced pressure to obtain 0.115 g of the target compound 119hydrocholoride (119 hydrochloride) in a 38.24% yield. ESI-MS: 238.18 (M+H) + . 1 H NMR(500MHz,Chloroform-d)δ2.79(d,J=12.4Hz,1H),2.59–2.52(m,6H),2.55–2.49(m,2H),2.41(d,J=12.5Hz,1H),1.81–1.74 (m,1H),1.67–1.59(m,2H),1.62–1.54(m,1H),1.57–1.49(m,1H),1.06(t,J=6.4Hz,8H),0.99(s,3H),0.95(s,3H),0.90(s,3H).

[0518] k2) Preparation of representative compound 115

[0519] Compound 119-1 (1.00 g, 5.10 mmol) was dissolved in 25 mL of dichloromethane, and HATU (2.91 g, 7.64 mmol) was added. The mixture was stirred at -10°C for 30 minutes, followed by the addition of 115-1 (447.23 mg, 6.11 mmol) and DIPEA (1.98 g, 15.29 mmol). The reaction was transferred to 40°C and allowed to react for 8 hours. TLC monitoring (PE:EA = 20:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was evaporated, and the sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA=50:1, v / v, yielded target intermediate 115-20.87 g, yield 67.92%. ESI-MS: 252.18 (M+H) + .

[0520] Compound 115-2 (0.87 g, 3.46 mmol) was dissolved in 25 mL of toluene, and 119-4 (257.78 mg, 4.15 mmol) was added. A water separator was installed and the reaction was refluxed at 120°C for 6 hours. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and the sample was mixed. The product was then purified by silica gel column chromatography using the developing solvent: PE:EA = 50:1, v / v. The target intermediate 115-3 was obtained in a yield of 73.35%. ESI-MS: 296.21 (M+H). + .

[0521] Compound 115-3 (0.75 g, 2.54 mmol) was dissolved in 25 mL of toluene, and 119-6 (615.88 mg, 3.05 mmol) was added. The reaction was continued at 60°C for 8 hours, monitored by TLC (PE:EA = 5:1, v / v, Rf = 0.3). After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, the sample was mixed, and the mixture was purified by silica gel column chromatography. Developing solvent: PE:EA = 10:1, v / v, yielding 0.52 g of the target compound 115-4 in a 72.78% yield. ESI-MS: 282.23 (M+H). + .

[0522] Compound 115-4 (0.52 g, 1.85 mmol) was dissolved in 25 mL of ethyl acetate, and a solution of HCl in 1,4-dioxane (dioxane hydrocholoride) 119-7 (67.525 mg, 1.85 mmol) was added. The mixture was allowed to react at 40°C for 8 hours. After completion of the reaction, the solvent was evaporated under reduced pressure to obtain 0.50 g of the target compound 115 hydrocholoride (115 hydrochloride) in an 85.10% yield. ESI-MS: 238.20 (M+H) + . 1H NMR(500MHz,Chloroform-d)δ3.00–2.90(m,1H),2.77(qd,J=13.9,4.0Hz,2H),2.40–2.30(m,2H),1.93(dt,J=6.6,4.0Hz,1H),1.78–1.71( m,1H),1.67–1.56(m,2H),1.54–1.46(m,1H),1.43(qd,J=7.4,4.0Hz,2H),1.14(d,J=5.6Hz,3H),0.97(d,J=17.9Hz,5H),0.94–0.88(m,6H).

[0523] k3) Preparation of representative compound 135

[0524] Compound 135-1 (0.50 g, 2.16 mmol) was dissolved in 25 mL of DMF, followed by the addition of 48-2 (0.7282 g, 6.49 mmol). The mixture was stirred at room temperature for 20 minutes, followed by the addition of 135-2 (0.1899 g, 2.60 mmol) and allowed to react at 50°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The combined organic phases were washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.24 g of the target compound 135 in a 49.67% yield. ESI-MS: 224.19 (M+1). + . 1 H NMR(500MHz,Chloroform-d)δ2.99–2.88(m,1H),2.38–2.27(m,2H),1.85–1.75(m,2H),1.65–1.55(m ,3H),1.44(qd,J=6.9,4.3Hz,2H),1.16(d,J=5.9Hz,3H),0.98(d,J=17.0Hz,5H),0.93–0.86(m,6H).

[0525] k4) Preparation of representative compound 138

[0526] Compound 135-1 (0.50 g, 2.16 mmol) was dissolved in 25 mL of DMF, followed by the addition of 48-2 (0.7282 g, 6.49 mmol). The mixture was stirred at room temperature for 20 minutes, followed by the addition of 138-2 (0.1899 g, 2.60 mmol) and allowed to react at 50°C for 8 hours. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.21 g of the target compound 138 in a 43.46% yield. ESI-MS: 224.19 (M+1). + . 1 H NMR(500MHz,Chloroform-d)δ2.55(qd,J=6.6,1.1Hz,4H),2.49–2.39(m,2H),1.93–1.84(m,1H),1 .84–1.74(m,2H),1.68–1.60(m,1H),1.07(t,J=6.7Hz,6H),1.02(s,2H),0.97(s,2H),0.92(s,2H).

[0527] 1) Preparation of Representative Compound 106

[0528] Compound 106-1 (0.20 g, 1.02 mmol) was dissolved in 25 mL of dichloromethane, and 106-3 (581.26 mg, 1.53 mmol) was added. The mixture was stirred at -10°C for 30 minutes, followed by the addition of 106-2 (86.98 mg, 1.22 mmol) and 106-4 (395.16 mg, 3.06 mmol). The reaction was then transferred to 40°C and allowed to react for 8 hours. TLC monitoring (PE:EA = 20:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA=50:1, v / v, yielding 0.068 g of target compound 106, with a yield of 26.76%. ESI-MS: 250.15 (M+H) + . 1H NMR(500MHz,Chloroform-d)δ6.55(d,J=6.2Hz,1H),3.79(dp,J=6.2,3.8Hz,1H),2.65(d,J=12.4Hz,1H) ,2.49(d,J=12.5Hz,1H),2.02–1.70(m,10H),1.63–1.52(m,4H),1.02(s,3H),0.98(s,3H),0.93(s,3H).

[0529] m1) Preparation of representative compound 157

[0530] Compound 157-1 (0.50 g, 2.55 mmol) was dissolved in 25 mL of glacial acetic acid, and ground 157-2 (622.00 mg, 5.61 mmol) was added. The mixture was heated to 120°C and refluxed for 24 h. TLC monitoring was performed (PE:EA = 2:1, v / v, Rf = 0.3). After completion of the reaction, the filter cake was washed twice with glacial acetic acid. The solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and distillation. The sample was mixed and then subjected to silica gel column chromatography. The eluent was PE:EA = 10:1, v / v. 0.38 g of the target intermediate 157-3 was obtained in a yield of 70.94%. ESI-MS: 209.20 (MH) - .

[0531] Compound 157-3 (0.38 g, 1.81 mmol) was dissolved in 25 mL of dichloromethane, and 157-5HATU (1.03 g, 2.71 mmol) was added. The mixture was stirred at -10°C for 30 minutes, followed by the addition of 157-4 (158.64 mg, 2.17 mmol) and 157-6DIPEA (700.86 mg, 5.42 mmol). The reaction was then transferred to 40°C and allowed to react for 8 hours. TLC monitoring (PE:EA = 20:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was evaporated, and the sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA=50:1, v / v, yielding 0.12 g of target compound 157, with a yield of 25.02%. ESI-MS: 266.14 (M+H) + . 1H NMR(500MHz,Chloroform-d)δ3.40(q,J=6.8Hz,4H),2.34(ddd,J=12.4,6.8,4.9Hz,1H),2.10(ddd,J=12.5,6.7,4.9Hz,1 H),1.97(ddd,J=12.3,6.8,4.9Hz,1H),1.77(ddd,J=12.4,6.8,4.9Hz,1H),1.23–1.13(m,8H),1.10(s,2H),1.05(s,2H).

[0532] m2) Preparation of representative compound 148

[0533] Compound 148-1 (0.50 g, 3.01 mmol) was dissolved in 25 mL of DMF, followed by the addition of 48-2 (0.7282 g, 6.49 mmol). The mixture was stirred at room temperature for 20 minutes, followed by the addition of 148-2 (0.4367 g, 3.61 mmol) and allowed to react at 50°C for 8 hours. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.35 g of the target compound 148 in a 56.40% yield. ESI-MS: 207.13 (M+1). + . 1 H NMR(500MHz,Chloroform-d)δ2.22(p,J=5.3Hz,0H),1.95–1.85(m,1H),1.73–1.55(m,1H),1.18(s,1H),1.03(s,1H),0.98(s,1H),0.59–0.45(m,2H).

[0534] m3) Preparation of representative compound 176

[0535] Compound 119-1 (1.00 g, 5.10 mmol) was dissolved in 25 mL of dichloromethane, and HATU (2.91 g, 7.64 mmol) was added. The mixture was stirred at -10°C for 30 minutes, followed by the addition of 176-1 (618.77 mg, 6.11 mmol) and DIPEA (1.98 g, 15.29 mmol). The reaction was transferred to 40°C and allowed to react for 8 hours. TLC monitoring (PE:EA = 20:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was evaporated, and the sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA=50:1, v / v, yielded target intermediate 176-20.58 g, yield 45.27%. ESI-MS: 294.17 (M+H) + .

[0536] Compound 176-2 (0.58 g, 2.31 mmol) was dissolved in 25 mL of toluene, and 119-4 (171.83 mg, 2.77 mmol) was added. A water separator was installed and the reaction was refluxed at 120°C for 6 hours. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, the sample was mixed, and the product was purified by silica gel column chromatography using the developing solvent: PE:EA = 50:1, v / v. 0.48 g of the target intermediate 176-3 was obtained in a yield of 70.42%. ESI-MS: 382.23 (M+H) + .

[0537] Compound 176-3 (0.48 g, 1.48 mmol) was dissolved in 25 mL of toluene, and 119-6 (359.98 mg, 1.78 mmol) was added. The reaction was continued at 60°C for 8 hours, monitored by TLC (PE:EA = 5:1, v / v, Rf = 0.3). After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and the sample was mixed. The mixture was then purified by silica gel column chromatography using the developing solvent: PE:EA = 10:1, v / v. The target compound 176-4 (0.36 g) was obtained in a 78.39% yield. ESI-MS: 368.26 (M+H) + .

[0538] Compound 176-4 (0.36 g, 1.16 mmol) was dissolved in 25 mL of ethyl acetate, and a solution of HCl in 1,4-dioxane (dioxane hydrocholoride 119-7) was added. The reaction was allowed to proceed at 40°C for 8 hours. After completion of the reaction, the solvent was evaporated under reduced pressure to obtain 0.27 g of the target compound 176 hydrocholoride (176 hydrochloride) in an 83.07% yield. ESI-MS: 280.21 (M+H) + . 1 H NMR(500MHz,Chloroform-d)δ3.02(d,J=12.8Hz,1H),2.84(d,J=12.6Hz,1H),2.47(t d,J=5.9,1.6Hz,4H),2.02(ddd,J=12.3,6.4,4.4Hz,1H),1.89(ddd,J=12.1,6.3,4.3 Hz,1H),1.79(ddd,J=12.3,6.2,4.4Hz,1H),1.64(ddd,J=12.3,6.4,4.4Hz,1H),1.48 (qt,J=7.8,5.9Hz,4H),1.18(s,2H),0.99(s,2H),0.94(s,2H),0.89(t,J=7.9Hz,6H).

[0539] m4) Preparation of representative compound 195

[0540] Compound 195-1 (1.00 g, 6.02 mmol) was dissolved in 25 mL of glacial acetic acid, and 195-2 (1.44 g, 9.02 mmol) and 195-3 (730.16 mg, 9.02 mmol) were added. The mixture was heated to 120°C and refluxed for 8 h. TLC monitoring (PE:EA = 2:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. The eluent was PE:EA = 10:1, v / v. 0.48 g of the target intermediate 195-4 was obtained in a yield of 32.55%. ESI-MS:245.00(M+1) + .

[0541] Compound 195-4 (0.48 g, 1.96 mmol) was dissolved in 25 mL of DMF, followed by the addition of 195-6 (0.6592 g, 5.87 mmol). The mixture was stirred at room temperature for 20 minutes, followed by the addition of 195-5 (0.1719 g, 2.35 mmol) and allowed to react at 50°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The combined organic phases were washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.27 g of the target compound 195 in 58.09% yield. ESI-MS: 238.17 (M+1). + . 1 H NMR(500MHz,Chloroform-d)δ2.78–2.61(m,4H),2.10–2.01(m,2H),1.90(ddd,J=11.9,6.6,5.0Hz,1 H),1.75(ddd,J=12.2,6.4,5.4Hz,1H),1.19(s,2H),1.11(t,J=6.7Hz,5H),1.04(s,2H),0.99(s,2H).

[0542] m5) Preparation of representative compound 212

[0543] The preparation of compound 195-4 was the same as compound 195.

[0544] Compound 195-4 (0.48 g, 1.96 mmol) was dissolved in 25 mL of DMF, followed by the addition of 195-6 (0.6592 g, 5.87 mmol). The mixture was stirred at room temperature for 20 minutes, followed by the addition of 212-1 (0.2706 g, 2.35 mmol), and the reaction was carried out at 50°C for 8 hours. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.38 g of the target compound 212 in a 69.46% yield. ESI-MS: 280.18 (M+1). + . 1H NMR(500MHz,Chloroform-d)δ3.73(dd,J=12.5,3.8Hz,2H),3.59(dd,J=12.4,3.9Hz,2H),3.32(qt,J=6.5,3.9Hz,2H),2.03(td,J =5.3,1.1Hz,2H),1.92(dt,J=12.3,5.4Hz,1H),1.70(ddd,J=12.3,5.8,4.8Hz,1H),1.21–1.16(m,8H),1.07(s,2H),1.02(s,2H).

[0545] m6) Preparation of representative compound 218

[0546] The preparation of compound 195-4 was the same as compound 195.

[0547] Compound 195-4 (0.48 g, 1.96 mmol) was dissolved in 25 mL of DMF, followed by the addition of 195-6 (0.6592 g, 5.87 mmol). The mixture was stirred at room temperature for 20 minutes, followed by the addition of 218-1 (0.1671 g, 2.35 mmol), and the reaction was carried out at 50°C for 8 hours. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.34 g of the target compound 218 in a 73.78% yield. ESI-MS: 236.15 (M+1). + . 1 H NMR(500MHz,Chloroform-d)δ2.86–2.75(m,4H),2.06–1.96(m,2H),1.90(dt,J=12.6,6.0Hz,1H ),1.83–1.77(m,2H),1.75(ddd,J=12.1,6.5,5.4Hz,1H),1.19(s,2H),1.04(s,2H),0.99(s,2H).

[0548] n) Preparation of representative compound 014

[0549] Compound 014-1 (200 mg, 1.31 mmol) was suspended in water, and 014-2 SelectFluor (511.94 mg, 1.45 mmol) was added. The mixture was stirred at 60°C under nitrogen for 8 hours. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, the sample was mixed, and silica gel column chromatography was performed. Developing solvent: PE:EA = 4:1, v / v, yielding 0.071 g of the target compound 014, with a yield of 31.75%. ESI-MS: 341.17 (2M+H) + . 1 H NMR (500MHz, Chloroform-d) δ2.52(dd,J=12.3,6.2Hz,1H),2.44(dd,J=12.5,6.2Hz,1H),2.17(dddd,J=25.3,12.4,10.1,7.3Hz,1H),2.08–1. 96(m,1H),1.99–1.91(m,1H),1.75(dddd,J=12.9,10.1,7.2,5.6Hz,1H) ,1.70(s,1H),1.62–1.54(m,1H),1.57–1.48(m,1H),0.70–0.48(m,4H).

[0550] o1) Preparation of representative compound 223

[0551] Compound 223-1 (0.50 g, 2.74 mmol) was dissolved in 25 mL of dichloromethane and stirred at -10°C for 20 minutes. Then, 223-2 (350.84 mg, 3.29 mmol) and 223-3TEA (833.01 mg, 8.23 ​​mmol) were added. The reaction mixture was transferred to 0°C and allowed to react for 8 hours. TLC monitoring (PE:EA = 20:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.37 g of the target compound 223 in a 56.58% yield. ESI-MS:253.13(M+H) + . 1H NMR(500MHz,Chloroform-d)δ4.36(d,J=1.2Hz,2H),3.25(tq,J=4.6,1.5Hz,1H),2.32(t,J=7.1Hz,2H),1.9 3–1.82(m,2H),1.81–1.71(m,1H),1.71–1.54(m,3H),1.19(s,2H),1.08(d,J=1.6Hz,3H),0.97–0.90(m,3H).

[0552] o2) Preparation of Representative Compound 229

[0553] Compound 223-1 (0.50 g, 2.74 mmol) was dissolved in 25 mL of dichloromethane and stirred at -10°C for 20 minutes. Compound 229-2 (462.85 mg, 3.29 mmol) and 223-3TEA (833.01 mg, 8.23 ​​mmol) were then added. The reaction mixture was transferred to 0°C and allowed to react for 8 hours. TLC monitoring (PE:EA = 20:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.31 g of the target compound 229 in a 41.48% yield. ESI-MS:287.12(M+H) + . 1 H NMR(500MHz,Chloroform-d)δ8.04–7.98(m,2H),7.58–7.51(m,1H),7.49–7.41(m,2H),4.47(d,J=1.8Hz,2H),3.25( tq,J=4.6,1.6Hz,1H),1.93–1.82(m,2H),1.81–1.70(m,1H),1.65–1.54(m,1H),1.19(s,2H),1.09(d,J=1.6Hz,3H).

[0554] o3) Preparation of Representative Compound 234

[0555] Compound 223-1 (0.50 g, 2.74 mmol) was dissolved in 25 mL of DMF, followed by the addition of 48-2 (0.6158 g, 5.49 mmol). The mixture was stirred at room temperature for 20 minutes, followed by the addition of 234-2 (0.4445 g, 3.29 mmol), and the reaction was carried out at 50°C for 8 hours. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.27 g of the target compound 234 in a 41.64% yield. ESI-MS: 237.14 (M+1). + . 1 H NMR(500MHz,Chloroform-d)δ3.55(d,J=11.7Hz,1H),3.50(d,J=11.7Hz,1H),3.34(dd,J=10.8,3.7Hz,1H),3.24(tq,J=4.8,1.5Hz,1H),3.18(dd,J=10.7 ,3.8Hz,1H),1.93–1.83(m,2H),1.80–1.68(m,1H),1.65–1.54(m,1H),1.18( s,2H),1.11(pt,J=6.4,3.8Hz,1H),1.03(d,J=1.4Hz,3H),0.38–0.23(m,4H).

[0556] o4) Preparation of Representative Compound 239

[0557] Compound 223-1 (0.50 g, 2.74 mmol) was dissolved in 25 mL of DMF, followed by the addition of 48-2 (0.9237 g, 8.23 ​​mmol). The mixture was stirred at room temperature for 20 minutes, followed by the addition of 239-2 (0.6766 g, 3.29 mmol), and the reaction was carried out at 50°C for 8 h. TLC monitoring (PE:EA = 30:1, v / v, Rf = 0.3) was performed. After completion of the reaction, 100 mL of saturated sodium chloride solution was added, followed by extraction with 100 mL of ethyl acetate (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration, and the sample was mixed and subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.28 g of the target compound 239 in a 33.26% yield. ESI-MS: 307.10 (M+1). + . 1H NMR(500MHz,Chloroform-d)δ7.34–7.28(m,2H),7.25(dt,J=8.0,1.1Hz,2H),4.53(t,J=1.0Hz,2H),3.64(s,2H),3.2 4(tq,J=4.8,1.5Hz,1H),1.93–1.83(m,2H),1.80–1.69(m,1H),1.65–1.54(m,1H),1.18(s,2H),1.03(d,J=1.4Hz,3H).

[0558] o5) Preparation of Representative Compound 245

[0559] Compound 223-1 (0.50 g, 2.74 mmol) was dissolved in 25 mL of dichloromethane and stirred at -10°C for 20 minutes. Then, 245-2 (462.90 mg, 3.29 mmol) and 223-3TEA (833.01 mg, 8.23 ​​mmol) were added. The reaction mixture was transferred to 0°C and allowed to react for 8 hours. TLC monitoring (PE:EA = 20:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.41 g of the target compound 245 in a 54.86% yield. ESI-MS:287.08(M+H) + . 1 H NMR (500MHz, Chloroform-d) δ4.05 (d, J=12.5Hz, 1H), 3.71–3.55 (m, 2H), 3.28 (tq, J=4. 8,1.6Hz,1H),1.93–1.83(m,2H),1.83–1.54(m,6H),1.19(s,2H),1.09(d,J=1.4Hz,3H).

[0560] o6) Preparation of Representative Compound 249

[0561] Compound 223-1 (0.50 g, 2.74 mmol) was dissolved in 25 mL of dichloromethane and stirred at -10°C for 20 minutes. Compound 249-2 (627.73 mg, 3.29 mmol) and 223-3TEA (833.01 mg, 8.23 ​​mmol) were then added. The reaction mixture was transferred to 0°C and allowed to react for 8 hours. TLC monitoring (PE:EA = 20:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v, yielding 0.35 g of the target compound 249 in a 39.56% yield. ESI-MS:337.10(M+H) + . 1 H NMR(500MHz,Chloroform-d)δ7.74–7.68(m,2H),7.40(dq,J=8.4,0.9Hz,2H),4.21(d,J=12.6Hz,1H),3.99(d,J=12.6Hz,1H),3.28(tq, J=4.9,1.5Hz,1H),2.41(d,J=0.9Hz,2H),1.93–1.83(m,2H),1.80–1.68(m,1H),1.64–1.54(m,1H),1.19(s,2H),1.09(d,J=1.4Hz,2H).

[0562] o7) Preparation of Representative Compound 257

[0563] Compound 223-1 (1.00 g, 5.49 mmol) was dissolved in 50 mL of dichloromethane and stirred at -10°C for 20 minutes. Then, 257-2 (4.66 g, 10.98 mmol) was added and the mixture was transferred to 0°C for 8 hours. TLC monitoring (PE:EA = 20:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then chromatographed on a silica gel column. Developing solvent: PE:EA = 50:1, v / v. 0.64 g of the target compound 257-3 was obtained in a 64.72% yield. ESI-MS: 181.06 (M+H) + .

[0564] Compound 257-3 (0.64 g, 3.55 mmol) was dissolved in 25 mL of tetrahydrofuran and stirred at -78°C for 20 minutes. Then, 257-4 (1.03 g, 7.10 mmol) was slowly added dropwise. The mixture was transferred to 0°C and allowed to react for 8 hours. TLC monitoring (PE:EA = 20:1, v / v, Rf = 0.3) was performed. After completion of the reaction, the solvent was evaporated under reduced pressure, and 100 mL of saturated sodium chloride solution was added. The mixture was then extracted with 100 mL of dichloromethane (100 mL x 3). The organic phases were combined, washed twice with 50 mL of pure water and twice with 50 mL of saturated sodium chloride solution, and dried over anhydrous magnesium sulfate. The solvent was removed by filtration and evaporated. The sample was mixed and then subjected to silica gel column chromatography. Developing solvent: PE:EA = 50:1, v / v. The target compound 257 (0.24 g) was obtained in a 30.40% yield. ESI-MS: 223.15 (M+H) + . 1 H NMR(500MHz,Chloroform-d)δ3.63(ddq,J=7.2,4.4,1.5Hz,1H),3.18(tq,J=4.5,1.5Hz,1H),2.94(d,J=4.4Hz,1H),1.94–1.83( m,2H),1.79–1.69(m,1H),1.69–1.60(m,1H),1.49(dp,J=6.8,5.0Hz,1H),1.20(s,2H),1.05(t,J=1.5Hz,3H),0.54–0.36(m,4H).

[0565] According to the similar method of the above example, the following example compounds in Table 1 were obtained:

[0566] Table 1. Compounds of the present invention

[0567] The beneficial effects of the compounds of the present invention are illustrated below by way of examples.

[0568] Test Example 1: Compounds improve respiratory function during inhalation general anesthesia with preserved spontaneous breathing

[0569] 1. Main reagents, equipment and drugs

[0570] (1) Main reagents

[0571] Kaitly (Approval No.: National Medicine Standard H20040772, Manufacturer: Jiangsu Hengrui Medicine Co., Ltd.). Medium / long chain fat emulsion injection (C 6～24 )(Approval number: National Medicine Standard H20030609, manufacturer: Huarui Pharmaceutical Co., Ltd.).

[0572] (2) Main equipment

[0573] Unrestrained whole-body plethysmography system (non-invasive respiratory measurement system) (Origin: United States, Manufacturer: DATA SCIENCES INTERNATIONAL).

[0574] (3) Test drug

[0575] The preparation method is as follows: weigh appropriate amounts of the test compounds respectively, add appropriate amounts of medium-chain triglyceride emulsion injection using a pipette to prepare a 4 mg / mL test compound solution, filter with a 0.22 μm microporous filter membrane, and use immediately.

[0576] 2. Experimental methods

[0577] Male Sprague-Dawley rats weighing 250-300 grams were randomly divided into groups of 6 rats each. Basal respiratory rate was recorded. Continuous anesthesia was induced with 2 MAC of sevoflurane and maintained with 1.5 MAC. Basal respiratory rate (average respiratory rate over 10 minutes) was recorded during anesthesia. The test drug was administered via the tail vein, and respiratory rate (average respiratory rate over 10 minutes) was observed and recorded.

[0578] The MAC value of an inhaled anesthetic is an important indicator for evaluating its performance. MAC, short for minimum alveolar concentration, is the concentration of the anesthetic in the alveolar air at atmospheric pressure (1 atmosphere) at which 50% of patients no longer experience a motor response to a noxious stimulus (such as skin incision). The unit is vol%.

[0579] 3. Experimental results

[0580] The results are shown in Table 2.

[0581] Table 2. Effects of the tested drugs on improving respiratory function during inhalation general anesthesia with preserved spontaneous breathing

[0582] The experimental results show that the compound of the present invention can improve the respiratory function during inhalation general anesthesia while retaining spontaneous breathing.

[0583] Test Example 2: Compounds Improve Respiratory Function in Opioid-Induced Respiratory Depression

[0584] 1. Main reagents and drugs

[0585] (1) Main reagents

[0586] Fentanyl citrate injection (approval number: National Medicine Standard H220003688, manufacturer: Yichang Renfu Pharmaceutical Co., Ltd.), oxidized camphor injection (approval number: National Medicine Standard H22025735, manufacturer: Changchun Changqing Pharmaceutical Group Co., Ltd.), sodium camphorsulfonate injection (approval number: National Medicine Standard H41023871, manufacturer: Anyang Jiuzhou Pharmaceutical Co., Ltd.).

[0587] (2) Main equipment

[0588] Unrestrained whole-body plethysmography system (non-invasive respiratory measurement system) (Origin: United States, Manufacturer: DATA SCIENCES INTERNATIONAL).

[0589] (3) Test drug

[0590] The preparation method is the same as that of Test Example 1.

[0591] 2. Experimental methods

[0592] Male Sprague-Dawley rats weighing 250-300 grams were randomly divided into groups of six. Baseline respiratory rate was recorded. 10 mg / kg fentanyl was administered via the tail vein, and the average respiratory rate was recorded for 10 minutes after opioid administration. The test drug was administered via the tail vein, and the average respiratory rate was recorded for 10 minutes after administration.

[0593] 3. Experimental results

[0594] Table 3. Improvement of opioid-induced respiratory depression by the tested drugs

[0595] The experimental results show that compared with sodium camphorsulfonate and oxidized camphor, the compound of the present invention can significantly improve respiratory depression induced by opioids at a lower dose.

[0596] Test Example 3: Determination of the minimum dose of a compound that causes severe adverse reactions

[0597] 1. Main reagents and drugs

[0598] (1) Main reagents

[0599] Oxidized camphor injection (approval number: National Medicine Standard H22025735, manufacturer: Changchun Changqing Pharmaceutical Group Co., Ltd.), sodium camphorsulfonate injection (approval number: National Medicine Standard H41023871, manufacturer: Anyang Jiuzhou Pharmaceutical Co., Ltd.).

[0600] (2) Test drug

[0601] The preparation method is the same as that of Test Example 1.

[0602] 2. Experimental methods

[0603] ICR mice weighing 20 ± 2 g, half male and half female, were randomly divided into groups of 10 mice each. The dose was increased in a geometric progression, with a ratio of 0.6 to 0.9:1 between adjacent doses. A single intravenous injection of the test drug was administered via the tail vein. The dose was administered from low to high. If adverse reactions occurred, the dose was reduced; otherwise, the dose was increased until the minimum dose that produced severe adverse reactions was found.

[0604] Table 4. Minimum dose determination of the test drug for serious adverse reactions

[0605] Note: The doses for serious adverse reactions in this table refer to the doses for any one of delirium, epileptic convulsions and dyspnea.

[0606] The experimental results show that compared with camphor oxide and sodium camphorsulfonate, the minimum dose for the occurrence of serious adverse reactions of the compounds of the present invention is generally higher and has higher safety.

[0607] In summary, the present invention provides the use of a cyclic ketone compound represented by formula I and a prodrug thereof in the preparation of a drug for improving respiratory depression caused by anesthetics and / or sedatives. The present invention discovered for the first time that the cyclic ketone compound and its prodrug can significantly improve respiratory depression caused by anesthetics and / or sedatives. Experimental results show that the compound of the present invention and its prodrug can improve respiratory function in inhaled general anesthesia with retained spontaneous breathing; at the same time, compared with sodium camphorsulfonate and oxidized camphor, the compound of the present invention can significantly improve respiratory depression induced by opioids at a lower dose, and the minimum dose that induces adverse reactions is higher and the safety is better. The present invention has a good improvement effect on respiratory depression caused by opioids and inhaled anesthetics, provides a new solution for respiratory depression caused by clinical anesthesia, and has broad application prospects.

Claims

1. A compound of formula I, or a stereoisomer thereof, or a deuterated derivative thereof, or a prodrug thereof, or a salt thereof, or a solvate thereof: in, n1 is 1 or 2; n is 0, 1 or 2; when n is 0, the connection between R6 and R4 and the connection between R3 and R4 If none, connect R6 and R3 When n is 1 or 2, the bond between R6 and R4 and between R3 and R4 As a key, connect R6 and R3 is a key or None; m is 0 or 1; when m is 0, the connection between R8 and R0 and the connection between R8 and R3 When m is 1, R8 and R0 are connected, and R8 and R3 are connected. is the key; Connect R3, R 10 , R7, R 11 of Depending on the number of bonds connecting the carbon atoms, it is either bonded or absent; R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 , -CR 12 =NR 13 , -CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form = NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L1, L2, L3, L4, L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x1 , R x2 , R x3 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x1 , R x2 , R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 11 Selected from hydrogen, deuterium, tritium, halogen, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl; R3, R 10 Each independently selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x4 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , = C(L 12 R X6 )(L 13 R X7 ), =O; or R4 and R5 or R6 and R7 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x5 , R x6 , R x7 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x5 , R x6 , R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R8 and R9 are each independently selected from -L 14 L 15 L 16 R X8 ; L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; said L 14 , L 15 , L 16 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x8 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x8 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 , R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, and 3- to 10-membered heterocycloalkyl.

2. The compound according to claim 1, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is shown in formula II: in, n is 0, 1 or 2; when n is 0, the connection between R6 and R4 and the connection between R3 and R4 If none, connect R6 and R3 When n is 1 or 2, the bond between R6 and R4 and between R3 and R4 As a key, connect R6 and R3 is a key or None; Connect R 10 、R7 Depending on the number of bonds connecting the carbon atoms, it is either bonded or absent; R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 , -CR 12 =NR 13 , -CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form = NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L1, L2, L3, L4, L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x1 , R x2 , R x3 are each independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or the following groups substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x1 , R x2 , R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 11 Selected from hydrogen, deuterium, tritium, halogen, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl; R3, R 10 Each independently selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x4 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , = C(L 12 R X6 )(L 13 R X7 ), =O; or R4 and R5 or R6 and R7 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x5 , R x6 , R x7 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x5 , R x6 , R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3-10 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 , R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl; Preferably, the compound is represented by formula II-1 or II-2:

3. The compound according to claim 1, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is shown in formula III: in, n is 0, 1 or 2; when n is 0, the connection between R6 and R4 and the connection between R3 and R4 If none, connect R6 and R3 When n is 1 or 2, the bond between R6 and R4 and between R3 and R4 As a key, connect R6 and R3 is a key or None; Connect R3 and R7 Depending on the number of bonds connecting the carbon atoms, it is either bonded or absent; R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, COR 12 、-COOR 12 , -OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 , -CR 12 =NR 13 , -CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form = NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L1, L2, L3, L4, L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x1 , R x2 , R x3 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x1 , R x2 , R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R3 is selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x4 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 Formation = NL 11 R X5 , = C(L 12 R X6 )(L 13 R X7 ), =O; or R4 and R5 or R6 and R7 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x5 , R x6 , R x7 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x5 , R x6 , R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R8 and R9 are each independently selected from -L 14 L 15 L 16 R X8 ; L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; said L 14 , L 15 , L 16 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x8 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x8 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 , R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, and 3- to 10-membered heterocycloalkyl.

4. The compound according to claim 3, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula III: The compound is represented by formula IIIa or IIIb: in, n, R0, R1, R2, R3, R4, R5, R6, R7, R8, R9 are as shown in claim 3.

5. The compound according to claim 2, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula IIa: in, R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 , -CR 12 =NR 13 , -CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form = NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L1, L2, L3, L4, L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x1 , R x2 , R x3 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x1 , R x2 , R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 11 Selected from hydrogen, deuterium, tritium, halogen, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl; R3 is selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x4 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R6 is selected from -L9L 10 L 11 R X5 ; L9, L 10 , L 11 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x5 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x5 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 , R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl; Preferably, the compound is represented by Formula IIa-1 or Formula IIa-2:

6. The compound according to claim 3, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula IIIa: in, R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 , -CR 12 =NR 13 , -CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form = NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L1, L2, L3, L4, L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x1 , R x2 , R x3 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x1 , R x2 , R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R6 is selected from -L9L 10 L 11 R X5 ; L9, L 10 , L 11 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x5 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x5 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R8 and R9 are each independently selected from -L 14 L 15 L 16 R X8 ; L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; said L 14 , L 15 , L 16 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x8 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x8 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 , R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, and 3- to 10-membered heterocycloalkyl.

7. The compound according to claim 6, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula IIIa1 or formula IIIa2: Among them, R0, R1, R2, R6, R8, and R9 are as shown in claim 6.

8. The compound according to claim 2, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula IIb: in, R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, COR 12 、-COOR 12 , -OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 , -CR 12 =NR 13 , -CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form = NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L1, L2, L3, L4, L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x1 , R x2 , R x3 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x1 , R x2 , R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 11 Selected from hydrogen, deuterium, tritium, halogen, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl; R3, R 10 Each independently selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x4 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , = C(L 12 R X6 )(L 13 R X7 ), =O; or R4 and R5 or R6 and R7 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x5 , R x6 , R x7 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x5 , R x6 , R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 , R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl; Preferably, the compound is represented by Formula IIb-1, Formula IIb-2, Formula IIb-3 or Formula IIb-4:

9. The compound according to claim 3, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula IIIb: in, R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 , -CR 12 =NR 13 , -CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form = NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L1, L2, L3, L4, L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x1 , R x2 , R x3 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x1 , R x2 , R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R3 is selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3-10 membered cycloalkyl, 3-10 6- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x4 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , = C(L 12 R X6 )(L 13 R X7 ), =O; or R4 and R5 or R6 and R7 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x5 , R x6 , R x7 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x5 , R x6 , R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R8 and R9 are each independently selected from -L 14 L 15 L 16 R X8 ; L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; said L 14 , L 15 , L 16 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x8 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x8 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 , R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, and 3- to 10-membered heterocycloalkyl.

10. The compound according to claim 9, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula IIIb1 or IIIb2: in, R0, R1, R2, R3, R4, R5, R6, R7, R8, and R9 are as shown in claim 9.

11. The compound according to claim 5, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula IIa1: in, R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 , -CR 12 =NR 13 , -CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 11 Selected from hydrogen, deuterium, tritium, halogen, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl; R3 is selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x4 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R6 is selected from -L9L 10 L 11 R X5 ; L9, L 10 , L 11 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x5 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x5 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 , R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl; Preferably, the compound is represented by formula IIa1-1 or IIa1-2:

12. The compound according to claim 11, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl; the substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro; R 11 Selected from hydrogen, deuterium, tritium, halogen; R3 is selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from the following groups: 1～6 Alkylene, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, -CO-, -NR 13 -、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy; R x4 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 alkyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl; said R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy; R6 is selected from -L9L 10 L 11 R X5 ; L9, L 10 , L 11 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, -CO-, -COO-, -OCO-, -O-, -S-, -SOO-, -NR 13 -、-CONR 13 -; L9, L 10 , L 11 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy; R x5 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 alkenyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl; said R x5 The substituents in independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy; R 12 , R 13 , R 14 , R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy.

13. The compound according to claim 8, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula IIb1, IIb2 or IIb3: in, R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 , -CR 12 =NR 13 , -CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form = NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L1, L2, L3, L4, L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x1 , R x2 , R x3 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x1 , R x2 , R x3 The substituents in Selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 11 Selected from hydrogen, deuterium, tritium, halogen, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl; R3, R 10 Each independently selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x4 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , = C(L 12 R X6 )(L 13 R X7 ), =O; or R4 and R5 or R6 and R7 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x5 , R x6 , R x7 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x5 , R x6 , R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 , R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl; Preferably, the compound is represented by formula IIb1-1, IIb1-2, IIb2-1, IIb2-2, IIb3-1, IIb3-2:

14. The compound according to claim 13, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: R0 is selected from the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl; the substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro; R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form = NL3R X1 , =C(L4R X2 )(L5R X3 ); or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L1, L2, L3, L4, L5 are each independently selected from the following groups: 1～6 Alkylene, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -O-, -S-, -SOO-, -NR 13 CO-、-NR 13 -、-CONR 13 -; the substituents in L1, L2, L3, L4, and L5 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy; R x1 , R x2 , R x3 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 alkyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl; said R x1 , R x2 , R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy; R 11 Selected from hydrogen, deuterium, tritium, halogen; R3, R 10 Each independently selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -NR 13 -、-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy; R x4 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy; R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , = C(L 12 R X6 )(L 13 R X7 ); L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, -CO-, -COO-, -OCO-, -O-, -S-, -SOO-, -NR 13 -、-CONR 13 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy; R x5 , R x6 , R x7 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 6-10 membered aryl; said R x5 , R x6 , R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy; R 12 , R 13 , R 14 , R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy.

15. The compound according to claim 9, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula IIIb1, IIIb2 or IIIb3: in, R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 , -CR 12 =NR 13 , -CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form = NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L1, L2, L3, L4, L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x1 , R x2 , R x3 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x1 , R x2 , R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R3 is selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x4 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, Cyano, Nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , = C(L 12 R X6 )(L 13 R X7 ), =O; or R4 and R5 or R6 and R7 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x5 , R x6 , R x7 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x5 , R x6 , R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R8 and R9 are each independently selected from -L 14 L 15 L 16 R X8 ; L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; said L 14 , L 15 , L 16 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x8 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x8 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 , R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, and 3- to 10-membered heterocycloalkyl.

16. The compound according to claim 15, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula IIIb11, formula IIIb12, formula IIIb21, formula IIIb22, formula IIIb31 or formula IIIb32: in, R0, R1, R2, R3, R4, R5, R6, R7, R8, and R9 are as shown in claim 15.

17. The compound according to claim 15 or 16, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: R0 is selected from the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl; the substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro; R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form = NL3R X1 , =C(L4R X2 )(L5R X3 ); or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L1, L2, L3, L4, L5 are each independently selected from the following groups: 1～6 Alkylene, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -O-, -S-, -SOO-, -NR 13 CO-、-NR 13 -、-CONR 13 -; the substituents in L1, L2, L3, L4, and L5 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x1 , R x2 , R x3 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl; said R x1 , R x2 , R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R3 is selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -CONR 13 -、-NR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x4 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl, 6-10 membered aryl, 5-10 membered heteroaryl; the R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , = C(L 12 R X6 )(L 13 R X7 ); L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, -CO-, -COO-, -OCO-, -O-, -S-, -SOO-, -NR 13 -、-CONR 13 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x5 , R x6 , R x7 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3-10 membered cycloalkyl, 6-10 membered aryl; said R x5 , R x6 , R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R8 and R9 are each independently selected from -L 14 L 15 L 16 R X8 ; L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl; said L 14 , L 15 , L 16 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x8 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy; said R x8 The substituents in The halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 , R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, and 3- to 10-membered heterocycloalkyl.

18. The compound according to any one of claims 1 to 17, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is not:

19. The compound according to claim 9, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is shown in formula IV: in, R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more Substituents substituted with the following groups: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 , -CR 12 =NR 13 , -CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form = NL3R X1 , =C(L4R X2 )(L5R X3 ); or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L1, L2, L3, L4, L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x1 , R x2 , R x3 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x1 , R x2 , R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 , R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl; The compound is not: Preferably, in, R0 is selected from C 1～6 alkyl; R1 is selected from hydrogen, deuterium, tritium, C 1～6 alkyl; R2 is selected from -L1L2L3R X1 ; L1, L2, L3 are each independently selected from none, -CO-, -O-, -SOO-, unsubstituted or substituted with one or two or more substituents. 1～6 Alkylene; the substituents in L1, L2, and L3 are each independently selected from hydroxyl groups; R x1 Selected from C 1～6 Alkyl, 3-10 membered cycloalkyl, 5-10 membered heteroaryl, 6-10 membered aryl which is unsubstituted or substituted with one or two or more substituents; said R x1 The substituents in are independently selected from halogen, C 1～5 Alkyl, C 1～5 Alkoxy.

20. The compound according to claim 19, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula IVa or IVb: Wherein, R0, R1, and R2 are as shown in claim 19.

21. The compound according to claim 19 or 20, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: -L1L2L3R X1 In the embodiment, the structure of -L1L2L3- is selected from none, R x1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, 3-6-membered cycloalkyl, thienyl, and phenyl which is unsubstituted or substituted with one or two or more substituents; said R x1 The substituents in are each independently selected from fluorine, chlorine, bromine, iodine, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, C 1～5 Alkoxy.

22. The compound according to claim 19 or 20, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is one of the following compounds:

23. The compound according to claim 15, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula V: in, R0 is selected from C 1～6 alkyl; R3 is selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from none, C 1～6 Alkylene, -CO-, -NR 13 -; R x4 Selected from the following groups: fluorine, unsubstituted or substituted by one or two or more substituents: C 1～6 alkyl, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl; said R x4 The substituents in are each independently selected from C 1～5 Alkyl; and when L6, L7, and L8 are all null, R x4 Not selected from methyl; R 13 Selected from hydrogen, deuterium, tritium, C 1～6 alkyl.

24. The compound according to claim 23, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula Va or formula Vb: Wherein, R0 and R3 are as shown in claim 23.

25. The compound according to claim 23 or 24, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: -L6L7L8R x4 In the embodiment, the structure of -L6L7L8- is selected from none, R x4 Selected from the following groups which are fluorine, unsubstituted or substituted by one or two or more substituents: methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, 3-6 membered cycloalkyl, The R x4 The substituents in are independently selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl and tert-butyl; and -L6L7L8R x4 When there is no x4 Not selected from methyl; R 13 Selected from hydrogen, deuterium, tritium, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl.

26. The compound according to claim 23 or 24, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is one of the following compounds:

27. The compound according to claim 8, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula VIa or VIb: in, R0 is selected from hydrogen, deuterium, tritium, F, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl; the substituents in R0 are each independently selected from hydrogen, deuterium, tritium, F, I, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy; R 11 Selected from hydrogen, deuterium, tritium, F, I, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl; R3, R 10 Each independently selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x4 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl; The compound is not: Preferably, in, R0 is selected from fluorine, C 1～6 alkyl; R 11 Selected from fluorine, C 1～6 alkyl; R3, R 10 Each independently selected from -L6L7L8R x4 ; -L6L7L8R x4 In the formula, the structure of -L6L7L8- is selected from none; R x4 Selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 2～6 alkenyl, 3-6 membered cycloalkyl; and R3, R 10 R x4 Not at the same time hydrogen; Preferably, the compound is represented by formula VIa-1, VIa-2, VIb-1 or VIb-2:

28. The compound according to claim 27, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: R0 is selected from fluorine, methyl; R 11 Selected from fluorine, methyl; R3, R 10 Each independently selected from -L6L7L8R x4 ; -L6L7L8R x4 In the formula, the structure of -L6L7L8- is selected from none; R x4 is selected from hydrogen, deuterium, tritium, methyl, isopropyl, cyclopropyl, isopropenyl; and R3, R 10 R x4 Not at the same time as hydrogen.

29. The compound according to claim 27 or 28, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is one of the following compounds:

30. The compound according to claim 5, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula VIIa or VIIb: in, R0 is selected from the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl; the substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, and nitro; R 11 Selected from hydrogen, deuterium, tritium, F, I, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl; R3 is selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x4 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl; The compound is not: Preferably, in, R0 is selected from fluorine, C 1～6 alkyl; R 11 Selected from fluorine, C 1～6 alkyl; R3 is selected from -L6L7L8R x4 ; -L6L7L8R x4 In the formula, the structure of -L6L7L8- is selected from none; R x4 Selected from C 1～6 alkyl; More preferably, the compound is represented by Formula VIIa-1, VIIa-2, VIIb-1 or VIIb-2:

31. The compound according to claim 30, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: R0 is selected from fluorine, methyl; R 11 Selected from fluorine, methyl; R3 is selected from -L6L7L8R x4 ; -L6L7L8R x4 In the formula, the structure of -L6L7L8- is selected from none; R x4 Selected from isopropyl.

32. The compound according to claim 30 or 31, or a stereoisomer thereof, or a deuterated derivative thereof, or a prodrug thereof, or a salt thereof, or a solvate thereof, characterized in that: The compound is one of the following compounds:

33. The compound according to claim 9, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula VIII: in, R0 is selected from the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl; the substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro; R9 is selected from -L 14 L 15 L 16 R X8 ; L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; said L 14 , L 15 , L 16 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x8 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x8 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3-10 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl; The compound is not: Preferably, in, R0 is selected from C 1～6 alkyl; R9 is selected from -L 14 L 15 L 16 R X8 ; L 14 , L 15 , L 16 Each independently selected from none, -O-, -CO-, -SOO-, unsubstituted or substituted by one or two or more substituents 1～6 Alkylene; said L 14 , L 15 , L 16 The substituents in are each independently selected from hydroxyl groups; R x8 Selected from C 1～6 Alkyl, 3-10-membered cycloalkyl, unsubstituted or substituted with one or two or more substituents phenyl; said R x8 The substituents in are independently selected from halogen, C 1～5 Alkyl, C 1～5 Alkoxy.

34. The compound according to claim 33, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula VIIIa or VIIIb: Wherein, R0 and R9 are as shown in claim 33.

35. The compound according to claim 33 or 34, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: -L 14 L 15 L 16 R X8 Medium, -L 14 L 15 L 16 -The structure is selected from none, R X8 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, 3-6-membered cycloalkyl, and phenyl which is unsubstituted or substituted with one or two or more substituents; said R x8 The substituents in are each independently selected from fluorine, chlorine, bromine, iodine, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, C 1～5 Alkoxy.

36. The compound according to claim 33 or 34, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is one of the following compounds:

37. The compound according to claim 9, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula IX: in, R0 is selected from the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl; the substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro; R3 is selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from the following groups: 1～6 Alkylene, C 3～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 7- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x4 Selected from hydrogen, deuterium, tritium, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 7- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x4 The substituents in are independently selected from hydrogen, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl; The compound is not: Preferably, in, R0 is selected from C 1～6 alkyl; R3 is selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from none, C 1～6 Alkylene, -CO-, -NR 13 -; R x4 Selected from 3-10 membered cycloalkyl, C 1～6 alkyl.

38. The compound according to claim 37, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by Formula IXa or Formula IXb: Wherein, R0 and R3 are as shown in claim 37.

39. The compound according to claim 37 or 38, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: -L6L7L8R x4 In the embodiment, the structure of -L6L7L8- is selected from none, R x4 It is selected from 3-6 membered cycloalkyl, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl and tert-butyl.

40. The compound according to claim 37 or 38, or a stereoisomer thereof, or a deuterated derivative thereof, or a prodrug thereof, or a salt thereof, or a solvate thereof, characterized in that: The compound is one of the following compounds:

41. The compound according to claim 15, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula X: in, R0 is selected from the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, 3-10 membered cycloalkyl, 3-10 membered heterocycloalkyl; the substituents in R0 are each independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro; R9 is selected from -L 14 L 15 L 16 R X8 ; L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; said L 14 , L 15 , L 16 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x8 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x8 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R 12 , R 13 , R 14 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl; The compound is not: Preferably, R0 is selected from C 1～6 alkyl; R9 is selected from -L 14 L 15 L 16 R X8 ; L 14 , L 15 , L 16 Each independently selected from none, -CO-, -O-, -SOO-, unsubstituted or substituted by one or two or more substituents 1～6 Alkylene; said L 14 , L 15 , L 16 The substituents in are each independently selected from hydroxyl groups; R x8 Selected from C 1～6 Alkyl, 3-6 membered cycloalkyl, unsubstituted or substituted with one or two or more substituents phenyl; said R x8 The substituents in are each independently selected from fluorine, chlorine, bromine, iodine, C 1～5 Alkyl, C 1～5 Alkoxy.

42. The compound according to claim 41, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, characterized in that: The compound is represented by formula Xa or formula Xb: Among them, R0 and R9 are as shown in claim 41.

43. The compound according to claim 41 or 42, or a stereoisomer thereof, or a deuterated derivative thereof, or a prodrug thereof, or a salt thereof, or a solvate thereof, characterized in that: -L 14 L 15 L 16 R X8 Medium, -L 14 L 15 L 16 -The structure is selected from none, R X8 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, 3-6-membered cycloalkyl, and phenyl which is unsubstituted or substituted with one or two or more substituents; said R x8 The substituents in are each independently selected from fluorine, chlorine, bromine, iodine, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, C 1～5 Alkoxy.

44. The compound according to claim 41 or 42, or a stereoisomer thereof, or a deuterated derivative thereof, or a prodrug thereof, or a salt thereof, or a solvate thereof, characterized in that: The compound is one of the following compounds:

45. A prodrug of a compound represented by formula XI, or a stereoisomer thereof, or a deuterated derivative thereof, or a salt thereof, or a solvate thereof: R1' and R2' are connected to form a 3-10-membered cycloalkyl substituted by n' R3's, a 3-10-membered heterocycloalkyl substituted by n' R3's, a 6-10-membered aryl substituted by n' R3's, or a 5-10-membered heteroaryl substituted by n' R3's; or R1' and R2' are connected to form n' is an integer selected from 0 to 8; R3' is selected from C1-C8 alkyl, C1-C8 alkoxy, halogen, hydroxy, nitro, amino, cyano, -C(O)OR5', -C(O)R5'; R5' is selected from hydrogen, C1-C8 alkyl; L'Selected n1', n2', n3' are independently selected from integers of 0 to 8; and any carbon atom on the main chain of n1', n2', n3' is replaced by a heteroatom or not; the heteroatom is O, N or S; Each R6', R7', R8', R9', R 10 '、R 11 '、R 12 'are independently selected from hydrogen, C1~C8 alkyl; Ring A is selected from 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, and 5- to 10-membered heteroaryl; R 13 ' is a substituent on ring A, n4' is R 13 '; n4' is an integer selected from 0 to 8; Each R 13 'are independently selected from C1~C8 alkyl, C1~C8 alkoxy, halogen, hydroxyl, nitro, amino, cyano; R4' is selected from a' R 14 'substituted 3-10 membered cycloalkyl, with a' R 14 'substituted 3-10 membered heterocycloalkyl, with a' R 14 'substituted 6-10 membered aryl, with a' R 14 'Substituted 5- to 10-membered heteroaryl, -C(O)NR d3 R d4 、 a' is an integer selected from 0 to 8; Each R4' is independently selected from C1-C8 alkyl, C1-C8 alkoxy, halogen, hydroxyl, nitro, amino, cyano, -C(O)OR 15 ',-C(O)R 15 '、-O(CH2) b’ R 15 '; R 15 ' is selected from hydrogen, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, (CH2) c’ C(O)R 16 ', by p' R 17 'Substituted 6- to 10-membered aryl; b' and c' are independently selected from integers from 0 to 8; R 16 ' is selected from hydrogen, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl; p' is an integer selected from 0 to 8; Each R 17 'are independently selected from C1~C8 alkyl, C1~C8 alkoxy, halogen, hydroxyl, nitro, amino, cyano; R d1 , R d2 , R d3 , R d4 are independently selected from hydrogen, C1-C8 alkyl; n1, n, m, R0, R1, R2, R3, R4, R5, R6, R7, R8, R9, R 10 , R 11 As shown in any one of claims 1 to 44.

46. ​​A compound represented by formula XII, or a stereoisomer thereof, or a deuterated derivative thereof, or a prodrug thereof, or a salt thereof, or a solvate thereof: in, m is 0 or 1; when m is 0, the connection between R8 and R0 and the connection between R8 and R3 When m is 1, R8 and R0 are connected, and R8 and R3 are connected. is the key; Connect R1 and R4 is a key or None; Connect R 10 , R5, R2, R7, R 11 of Depending on the number of bonds connecting the carbon atoms, it is either bonded or absent; R0 is selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, the following groups which are unsubstituted or substituted by one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, COR 12 、-COOR 12 、-OCOR 12 、-OCOOR 12 -、-OR 12 、-SR 12 、-SOR 12 、-SOOR 12 、-NR 13 COR 12 、-NR 12 R 13 , -CR 12 =NR 13 , -CR 12 R 13 NR 14 R 15 、-NR 13 CSR 12 、-CONR 12 R 13 The substituents in R0 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, -NR 12 R 13 , 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R1 and R2 are each independently selected from -L1L2L3R X1 ; or R1 and R2 form = NL3R X1 , =C(L4R X2 )(L5R X3 ), =O; or R1 and R2 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L1, L2, L3, L4, L5 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L1, L2, L3, L4, and L5 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x1 , R x2 , R x3 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x1 , R x2 , R x3 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R3, R 10 Each independently selected from -L6L7L8R x4 ; L6, L7, L8 are each independently selected from the following groups: 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; the substituents in L6, L7, and L8 are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x4 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x4 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R4, R5, R6, and R7 are each independently selected from -L9L 10 L 11 R X5 ; or R4 and R5 or R6 and R7 form =NL 11 R X5 , = C(L 12 R X6 )(L 13 R X7 ), =O; or R4 and R5 or R6 and R7 are connected to form a 3-10 membered carbocyclic ring or a 3-10 membered carbocyclic ring; L9, L 10 , L 11 , L 12 , L 13 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; L9, L 10 , L 11 , L 12 , L 13 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x5 , R x6 , R x7 Each is independently selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, and the following groups which are unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x5 , R x6 , R x7 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R8 and R9 are each independently selected from -L 14 L 15 L 16 R X8 ; L 14 , L 15 , L 16 Each independently selected from the following groups which are absent, unsubstituted or substituted by one or two or more substituents: C 1～6 Alkylene, C 2～6 Alkenylene, C 2～6 Alkyne, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -CO-, -COO-, -OCO-, -OCOO-, -O-, -S-, -SO-, -SOO-, -NR 13 CO-、-NR 13 CS-、-NR 13 -、-CR 12 =N-,-CONR 13 -、-CR 12 R 13 NR 14 -; said L 14 , L 15 , L 16 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl; R x8 Selected from hydrogen, deuterium, tritium, halogen, cyano, nitro, unsubstituted or substituted with one or two or more substituents: C 1～6 Alkyl, C 1～6 Alkoxy, C 2～6 Alkenyl, C 2～6 Alkynyl, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered aryl, 5- to 10-membered heteroaryl, -N=NR 12 , -CR 12 =NR 13 ; said R x8 The substituents in are independently selected from hydrogen, deuterium, tritium, halogen, hydroxyl, cyano, nitro, C 1～5 Alkyl, C 1～5 Alkoxy, 3- to 10-membered cycloalkyl, 3- to 10-membered heterocycloalkyl, 6- to 10-membered Yuanaryl group, 5-10 yuan heteroaryl group; R 11 Selected from hydrogen, deuterium, tritium, halogen, C 1～6 Alkyl, C 2～6 Alkenyl, C 2～6 Alkynyl; R 12 , R 13 , R 14 , R 15 are each independently selected from hydrogen, deuterium, tritium, C 1～6 Alkyl, C 1～6 Alkoxy, 3- to 10-membered cycloalkyl, and 3- to 10-membered heterocycloalkyl.

47. Use of a compound according to any one of claims 1 to 44, or a stereoisomer, or a deuterated derivative, or a prodrug, or a salt, or a solvate thereof, or a prodrug of a compound of formula XI according to claim 45, or a stereoisomer, or a deuterated derivative, or a salt, or a solvate thereof, or a compound of formula XII according to claim 46, or a stereoisomer, or a deuterated derivative, or a prodrug, or a salt, or a solvate thereof, in the preparation of a medicament for improving respiratory function in inhalation general anesthesia with retained spontaneous breathing.

48. The use according to claim 47, characterized in that: The inhalation general anesthesia refers to anesthesia induced and maintained by isoflurane, sevoflurane, desflurane, enflurane, enflurane, and nitrous oxide.

49. Use of a compound according to any one of claims 1 to 44, or a stereoisomer, or a deuterated derivative, or a prodrug, or a salt, or a solvate thereof, or a prodrug of a compound of formula XI according to claim 45, or a stereoisomer, or a deuterated derivative, or a salt, or a solvate thereof, or a compound of formula XII according to claim 46, or a stereoisomer, or a deuterated derivative, or a prodrug, or a salt, or a solvate thereof in the preparation of a drug for improving respiratory function in respiratory depression induced by opioid overdose.

50. The use according to claim 49, characterized in that: The opioid drugs are morphine, fentanyl, sufentanil, remifentanil, alfentanil, carfentanil and other fentanyl derivatives, pethidine, tramadol, dezocine, pentazocine, hydromorphone, oxycodone, buprenorphine, butorphanol, and nalbuphine.

51. An anesthetic and / or sedative antagonist, characterized in that: It is a preparation prepared by using the compound described in any one of claims 1 to 44, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate, or the prodrug of the compound represented by formula XI described in claim 45, or its stereoisomer, or its deuterated derivative, or its salt, or its solvate, or the compound represented by formula XII described in claim 46, or its stereoisomer, or its deuterated derivative, or its prodrug, or its salt, or its solvate as the active ingredient, and adding pharmaceutically acceptable excipients.

52. The anesthetic and / or sedative antagonist according to claim 51, characterized in that: The preparation is a tablet, capsule, oral liquid, granule, pill, powder, injection or powder injection.

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