Brayaconitine A derivative having analgesic activity, method of preparation thereof, and use

Abstract

This invention discloses a breiaconitine A derivative having analgesic activity, a method for preparing the same, and its use, relating to the field of medicinal chemistry. A breiaconitine A derivative is a compound represented by formula (I), its isomer, its deuterated compound, its solvate, its prodrug, its metabolite, its crystalline form, or its pharmaceutically acceptable salt. The breiaconitine A derivatives provided in this invention have advantages such as high analgesic activity, good anti-inflammatory activity, low toxicity, high therapeutic index, and high water solubility, and can be applied to the preparation of low-toxicity, highly effective, and independent anti-inflammatory analgesics. [Formula 1] TIFF2026511621000134.tif45170 Formula I

Description

[Technical Field]

[0001] This invention belongs to the field of medicinal chemistry and specifically relates to a breiaconitine A derivative having analgesic activity, a method for preparing the same, and its use. [Background technology]

[0002] Pain is one of the diseases that harm human health. Chronic pain, also known as "non-dead cancer," has a serious impact on people's physical and mental health and quality of life, and is a major challenge in the global health field.

[0003] Bulleaconitine A, also known as crude uberlotin, is a C19-diterpenoid alkaloid distributed in most plants of the genus Aconitum, primarily found in Citropira (Aconitum L. bulleyanum Diels), a plant of the genus Aconitum. In 1986, scientists confirmed the analgesic effect of bulleaconitine A using the rising method, hot plate method, photothermal feeding method, and formaldehyde seizure method, and developed it as a clinical drug. Currently available dosage forms include tablets, capsules, pills, and injections. Oxalistatin has good analgesic, anti-inflammatory, and immunosuppressive effects and is widely used to treat various chronic pains such as rheumatoid arthritis, osteoarthritis, neuropathic pain, herpes zoster pain, shoulder pain, lumbar sprains, sprains, cancer pain, and postoperative pain. Furthermore, it can alleviate inflammatory responses such as redness, emphysema, and fever associated with rheumatoid arthritis and rheumatoid arthritis. Its non-dependency, drug tolerance, and gastrointestinal reactions result in significantly lower toxicity and side effects compared to opioids and nonsteroidal anti-inflammatory drugs, making it highly suitable for patients requiring long-term pain relief. In 2013, bryaconitine A was incorporated into the "Expert Consensus on Neuropathic Pain Management," demonstrating its important role in treating chronic pain caused by various factors. [ka] Braiaconitine A

[0004] Breiaconitine A is a non-addictive, non-opioid herbal analgesic with advantages such as high analgesic efficacy, long duration of action, and no dependence. However, it has a narrow safety margin and high acute toxicity, causing transient mild panic, nausea, numbness of the lips and tongue, and palpitations during use. Regarding the presentation of animal toxicity literature, the toxicity of the biester alkaloids contained in breiaconitine A is mainly to the nervous system (especially the vagus nerve and sensory nerves), and it also acts directly on the myocardium, potentially leading to death through respiration or myocardial paralysis. Therefore, developing new derivatives of breiaconitine A that have high biological activity and low toxicity is of great significance for the clinical application of analgesics. [Overview of the project]

[0005] The object of the present invention is to provide a breiaconitine A derivative with low toxicity and high analgesic activity, a method for preparing the same, and its use in pharmaceuticals.

[0006] The present invention provides compounds represented by the following formula I, their isomers, their deuterated compounds, their solvates, their prodrugs, their metabolites, their crystalline forms, or pharmaceutically acceptable salts thereof. [ka] Equation I (R1, R2, R3, R4, and R5 are independently hydrogen, hydroxyl, halogen, and C, respectively.) 1~18 Alkoxy, C 1~18 Alkyl, COOR a , OCOR a Selected from, R a is hydrogen, C 1~18 Selected from alkyl, phenyl, 3-6 member heteroaryl, 3-8 member saturated cycloalkyl, 3-8 member saturated heterocyclyl, condensed cycloalkyl, heterocondensed ring group, bicycloalkyl, and heterobicyclyl. R6 and R7 are independently hydrogen, hydroxyl, and C, respectively. 1~18 Alkoxy, C 1~18 Alkyl, OCORb 、OCOCH2R b 、OSO2R b selected from R b is hydrogen, C z alkyl substituted with one or more R 1~6 、C z alkenyl substituted with one or more R 2~6 、C z alkynyl substituted with one or more R 2~6 、phenyl substituted with one or more R z 、3- to 6-membered heteroaryl substituted with one or more R z 、3- to 8-membered saturated cycloalkyl substituted with one or more R z 、3- to 8-membered saturated heterocyclyl substituted with one or more R z 、fused cycloalkyl substituted with one or more R z 、hetero-fused ring group substituted with one or more R z 、bicycloalkyl substituted with one or more R z 、heterobicyclyl substituted with one or more R z selected from said R z is each independently hydrogen, substituted or unsubstituted C 1~6 alkyl, C 2~6 alkenyl, C 2~6 alkynyl, substituted or unsubstituted C 1~6 alkoxy, 3- to 8-membered saturated cycloalkyl, NR3R4, COOR5, SO2R6, halogen, cyano, nitro, hydroxyl, carboxyl, phenyl, and the substituents of said C 1~6 alkyl, C 1~6 alkoxy are selected from halogen, cyano, nitro, hydroxyl, carboxyl. )

[0007] Furthermore, the structure of said compound is represented by the following formula II.

Chemical formula

[0008] The structure of the aforementioned compound is represented by the following formula III. [ka] Formula III (In the formula, R6 and R7 are independently hydrogen, hydroxyl, and C, respectively) 1~6 Alkoxy, C 1~6 Alkyl, OCOR b OCOCH2R b OSO2R b Selected from, R b is hydrogen, one or more R z C replaced by 1~6 Alkyl, one or more R z C replaced by 2~6 Alkenyl, one or more R z C replaced by 2~6 Alkinyl, one or more R z Phenyl substituted with, one or more R z A 3-6 member heteroaryl substituted with one or more R z A 3- to 8-membered saturated cycloalkyl group substituted with one or more R z A 3- to 8-membered saturated heterocycline substituted with one or more R z A condensed cycloalkyl group substituted with one or more R z A heterocondensed ring group substituted with, one or more R z Bicycloalkyl substituted with, one or more R z Selected from heterobisicrills substituted with, The aforementioned R zis independently hydrogen, halogenated or non-halogenated C 1~6 alkyl, C 2~6 alkenyl, C 2~6 alkynyl, halogenated or non-halogenated C 1~6 alkoxy, 3-8 member saturated cycloalkyl, NR3R4, COOR5, SO2R6, halogen, cyano, nitro, hydroxyl, carboxyl, phenyl, R3 and R4 are independently hydrogen, C 1~6 alkyl, R5 is C 1~6 alkyl selected therefrom.)

[0009] Furthermore, the structure of the compound is represented by the following formula IV. [Chemical formula] Formula IV (In the formula, R6 and R7 are independently hydrogen, hydroxyl, C 1~6 alkoxy, C 1~6 alkyl, OCOR b , OCOCH2R b , OSO2R b selected from, R b is hydrogen, C substituted with one or more R z alkyl, C substituted with one or more R 1~6 alkenyl, C substituted with one or more R z alkynyl, phenyl substituted with one or more R 2~6 , 3-6 member heteroaryl substituted with one or more R z , 3-8 member saturated cycloalkyl substituted with one or more R 2~6 , 3-8 member saturated heterocyclyl substituted with one or more R z , fused cycloalkyl substituted with one or more R z , hetero-fused ring group substituted with one or more R z , 3-8 member saturated cycloalkyl substituted with one or more R z , 3-8 member saturated heterocyclyl substituted with one or more R z , fused cycloalkyl substituted with one or more R z , hetero-fused ring group substituted with one or more R zBicycloalkyl substituted with, one or more R z Selected from heterobisicrills substituted with, The aforementioned R z These are, independently, hydrogen, halogenated, or non-halogenated C. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkynyl, halogenated, or non-halogenated C 1~6 Selected from alkoxy, 3-8 member saturated cycloalkyl, NR3R4, COOR5, SO2R6, halogen, cyano, nitro, hydroxyl, carboxyl, and phenyl. R3 and R4 are hydrogen and C, respectively, independently. 1~6 Selected from alkyl, R5 is C 1~6 Selected from alkyl groups.

[0010] Furthermore, the structure of the compound is represented by the following formula V. [ka] Formula V (In the formula, R6 and R7 are independently hydrogen, hydroxyl, and C, respectively) 1~6 Alkoxy, C 1~6 Alkyl, OCOR b OCOCH2R b OSO2R b Selected from, R b is hydrogen, one or more R z C replaced by 1~6 Alkyl, one or more R z C replaced by 2~6 Alkenyl, one or more R z C replaced by 2~6 Alkinyl, one or more R z Phenyl substituted with, one or more R z A 3-6 member heteroaryl substituted with one or more R z A 3- to 8-membered saturated cycloalkyl group substituted with one or more R z A 3- to 8-membered saturated heterocycline substituted with one or more R zA condensed cycloalkyl group substituted with one or more R z A heterocondensed ring group substituted with, one or more R z Bicycloalkyl substituted with, one or more R z Selected from heterobisicrills substituted with, The aforementioned R z These are, independently, hydrogen, halogenated, or non-halogenated C. 1~6 Alkyl, C 2~6 Alkenil, C 2~6 Alkynyl, halogenated, or non-halogenated C 1~6 Selected from alkoxy, 3-8 member saturated cycloalkyl, NR3R4, COOR5, SO2R6, halogen, cyano, nitro, hydroxyl, carboxyl, and phenyl. R3 and R4 are hydrogen and C, respectively, independently. 1~6 Selected from alkyl, R5 is C 1~6 Selected from alkyl groups.

[0011] Furthermore, the structure of the compound is selected from the following structures. [ka] TIFF2026511621000009.tif253170TIFF2026511621000010.tif248170TIFF2026511621000011.tif252170 TIFF2026511621000012.tif239170TIFF2026511621000013.tif241170TIFF2026511621000014.tif130170

[0012] The present invention further provides a pharmaceutical composition for analgesia and / or anti-inflammatory purposes, comprising the above-mentioned compound, its isomer, its deuterated compound, its solvate, its prodrug, its metabolite, its crystalline form, or a pharmaceutically acceptable salt thereof as an active ingredient, and further comprising a pharmaceutically acceptable adjuvant.

[0013] The present invention further provides for the use of the above-mentioned compounds, their isomers, their deuterated compounds, their solvates, their prodrugs, their metabolites, their crystalline forms, or their pharmaceutically acceptable salts in the preparation of analgesic and / or anti-inflammatory agents.

[0014] Furthermore, the analgesic and / or anti-inflammatory agent is a low-toxicity analgesic and / or anti-inflammatory agent.

[0015] Furthermore, the median lethal dose of the aforementioned analgesic and / or anti-inflammatory drug is higher than that of breiaconitine A.

[0016] Furthermore, the therapeutic index of the analgesic and / or anti-inflammatory drug is higher than that of bryaconitine A.

[0017] This invention uses bikhaconine A as a semi-synthetic raw material and yields different bikhaconine AC19 diterpene alkaloid derivatives through various synthetic reactions. The method for preparing bikhaconine AC19 diterpene alkaloid derivatives is simple, requires mild conditions, and is suitable for large-scale production. The prepared diterpene alkaloid derivatives have the advantages of high analgesic activity, high anti-inflammatory activity, low toxicity, and a high therapeutic index. Furthermore, these diterpene alkaloids have advantages such as being non-addictive as an analgesics and not irritating the gastrointestinal tract, and are expected to have a wide range of applications as low-toxicity, highly effective, and non-addictive analgesics.

[0018] The compounds and derivatives provided in this invention are named according to the IUPAC (International Union of Pure and Applied Chemistry) or CAS (Chemical Abstracts Service) nomenclature.

[0019] In this invention, unless otherwise specified, the initial definitions of terms provided by a base or term herein constitute the entirety of that base or term in the specification, and terms not specifically defined in the text should be given the meaning that a person skilled in the art would give them based on the disclosure and context.

[0020] In the compound represented by formula I of the present invention, the minimum and maximum carbon content in the carbon-hydrogen group are represented by a prefix, for example, prefix C. a~b Alkyl refers to any alkyl group containing carbon atoms from "a" to "b". For example, C 1~6 Alkyl refers to a linear or branched alkyl group containing 1 to 6 carbon atoms.

[0021] "Substitution" means that one, two, or more hydrogen atoms in a molecule are replaced by other different atoms or molecules, and includes one, two, or more substitutions on isotopes or heteroatoms in the molecule.

[0022] "Cycloalkyl" refers to saturated or unsaturated cyclic hydrocarbon substituents. For example, "3-8 membered saturated cycloalkyl" refers to a saturated cycloalkyl group with 3 to 8 carbon atoms in the ring.

[0023] A "heterocyclyl" refers to a saturated or unsaturated cyclic hydrocarbon substituent, where a cyclic hydrocarbon contains at least one ring heteroatom (including, but not limited to, O, S, or N). For example, a "3- to 8-membered saturated heterocyclyl" means a saturated heterocyclyl with 3 to 8 ring atoms.

[0024] The term "aryl group" refers to a monocyclic group of all carbon atoms that has a conjugated π-electron system, such as phenyl.

[0025] "Heteroaryl" refers to a heteroaromatic group containing multiple heteroatoms. These heteroatoms include oxygen, sulfur, and nitrogen. Examples include furyl, thienyl, pyridyl, pyrazolyl, pyrrolyl, N-alkylpyrrolyl, pyrimidyl, pyrazinyl, imidazolyl, and tetrazolyl groups.

[0026] A "deuterated compound" is a compound in which one or more hydrogen atoms are substituted with deuterium.

[0027] "Bicycloalkyl" refers to a polycyclic cycloalkyl group in which two rings are linked by a single bond. For example, [ka] These are some examples.

[0028] A "heterobicyryl" refers to a polycyclic group in which two rings are joined by a single bond, and each ring contains at least one heterocycle. For example, [ka] These are some examples.

[0029] A "condensed cycloalkyl" refers to a polycyclic cycloalkyl group in which two rings share two adjacent carbon atoms. For example, [ka] These are some examples.

[0030] A "heterocondensed ring group" refers to a polycyclic group in which two rings share two adjacent carbon atoms, and each of the two rings contains at least one heteroring. For example, [ka] These are some examples.

[0031] Halogens refer to fluorine, chlorine, bromine, and iodine.

[0032] "Pharmacologically acceptable" means that a carrier, recipient, diluent, adjuvant, and / or a salt formed thereon is typically chemically or physically compatible with other components of a drug dosage form and physiologically compatible with the receptor.

[0033] "Salt" refers to acidic and / or basic salts formed by a compound or its stereoisomers with inorganic and / or organic acids and / or bases, including zwitterionic salts (inner salts), and also includes quaternary ammonium salts, such as alkylammonium salts. These salts can be obtained directly in the final separation and purification of the compound. They can also be obtained by appropriately (e.g., equimolarly) mixing the compound or its stereoisomers with a certain number of acids or bases. These salts can be produced by forming a precipitate in solution and collecting it by filtration, recovering it after evaporation of the solvent, or freeze-drying after reaction in an aqueous medium.

[0034] The pharmaceutically acceptable salts described in the present invention may be hydrochloride, sulfate, citrate, benzenesulfonate, hydrobromide, hydrofluoride, phosphate, acetate, propionate, succinate, oxalate, malate, succinate, fumarate, maleate, tartrate or trifluoroacetate of the compound.

[0035] Based on the above content of the present invention, it is obvious that those skilled in the art can make various other forms of modifications, substitutions or changes according to their knowledge and common means without departing from the above basic technical idea of the present invention.

[0036] Hereinafter, the above content of the present invention will be further described in more detail by specific embodiments of the embodiment form. However, it should not be understood that the scope of the above subject matter of the present invention is limited to the following examples. Any technology realized based on the above content of the present invention belongs to the scope of the present invention.

Embodiments for Carrying Out the Invention

[0037] The raw materials and equipment used in the present invention are known products and can be obtained by purchasing commercially available products.

[0038] Synthesize the target compound of the present invention according to the following route. Route 1

Chemical Formula

[0039] Route 2

Chem.

[0040] Example 1: Preparation of Compound 1 Weighed 1 g of brachyaconitine A and placed it in a 500 mL round-bottom flask, added 250 ml of methanol, heated it to reflux in an oil bath, detected the progress of the reaction by thin-layer chromatography, stopped the reaction after 24 h, rotary-evaporated the reaction solution, and separated and purified it by column chromatography to obtain the target compound. Its structure and characteristics are as follows.

Chem.

[0041] Example 2: Preparation of Compound 2 1 g of breiaconitine A was weighed and placed in a 500 mL round-bottom flask. 250 ml of ethanol was added, and the mixture was heated in an oil bath under reflux. The progress of the reaction was detected by thin-layer chromatography. After 72 hours, the reaction was stopped, the reaction mixture was evaporated by rotation, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 35 H 51 NO9, light yellow solid (550mg), yield 56.2%. HRESIMS m / z:[(M+H) + ,630.37] 1 H NMR (400MHz, CDCl3) δ8.01(d,J=8.8Hz,2H),6.89(d,J=8.8Hz,2H),4.82(d,J=5.2Hz,1H),3.99(d,J=6.6Hz,1H),3.84(s,3H),3.81(s,1H) ,3.60(d,J=8.2Hz,1H),3.51(s,3H),3.38(t,J=7.6Hz,1H),3.32(t,J=7.6Hz,1H),3.28(s,3H),3.24(d,J=2.2Hz,6H),3.11(dd,J=13.2,7 .8Hz,2H),3.02(dd,J=9.8,6.2Hz,1H),2.77(s,1H),2.70(s,1H),2.68-2.63(m,1H),2.49(s,3H),2.34(s,1H),2.31-2.26(m,2H),2.11-2 .01(m,3H),1.94-1.87(m,1H),1.63(dd,J=10.0,4.2Hz,2H),1.41(s,1H),1.32-1.26(m,1H),1.07(t,J=7.2Hz,3H),0.58(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ166.45,163.19,131.85,131.85,123.47,113.51,113.51,85.53,84.16,83.04,80.24,79.25,78.16,75.50,61.52,59 .14,58.85,58.82,56.46,55.94,55.47,53.91,50.71,49.27,49.11,4 8.48,46.52,41.49,39.15,37.38,36.60,35.02,26.46,15.41,13.58.

[0042] Example 3: Preparation of Compound 3 500 mg of compound 1 was weighed and placed in a 500 mL round-bottom flask. 120 mL of methanol solution containing 5% NaOH was added, and the mixture was reacted at 50°C. The reaction progress was detected by thin-layer chromatography. The reaction was allowed to proceed completely for 30 minutes. The reaction mixture was then evaporated by rotation, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 26 H 43 NO7, pale yellow solid (373 mg), yield 95.3%. HRESIMS m / z:[(M+H) + ,481.31] 1 H NMR(400MHz,Chloroform-d)δ5.29(s,1H),4.05(d,J=6.7Hz,1H),3.83(d,J=4.9Hz,1H),3.66(d, J=8.4Hz,1H),3.43(s,3H),3.36-3.33(m,1H),3.32(s,3H),3.30(s,3H),3.25(s,3H),3.22(s,3H) ),3.11(d,J=8.3Hz,1H),3.08-2.91(m,3H),2.59-2.39(m,6H),2.37-2.27(m,3H),2.26-2.21(m, 1H),2.09(d,J=6.6Hz,1H),1.96-1.85(m,3H),1.61(dd,J=9.6,3.9Hz,2H),1.08(t,J=7.1Hz,3H). 13 C NMR (101MHz, CDCl3) δ85.70,84.15,82.95,80.38,78.72,78.63,76.58,62.37,59.24,59.02,58.65,56. 46,53.68,50.56,49.77,49.32,49.21,48.91,48.39,41.80,39.34,36.44,35.48,34.13,26.27,13.74.

[0043] Example 4: Preparation of Compound 4 500 mg of compound 2 was weighed and placed in a 500 mL round-bottom flask. 120 ml of methanol solution containing 5% NaOH was added, and the mixture was reacted at 50°C. The reaction progress was detected by thin-layer chromatography, and the reaction was allowed to proceed completely for 30 minutes. The reaction mixture was then evaporated by rotation, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 27 H 45 NO7, pale yellow solid (368 mg), yield 93.6%. HRESIMS m / z:[(M+H) + ,496.34] 1 H NMR(400MHz,CDCl3)δ4.06(d,J=6.6Hz,1H),3.84(t,J=5.2Hz,1H),3.65(d, J=8.2Hz,1H),3.54-3.48(m,1H),3.48-3.43(m,1H),3.42(s,3H),3.32(dd, J=6.6,1.2Hz,1H),3.30(s,3H),3.29(s,3H),3.21(s,3H),3.11(d,J=5.8Hz ,1H),3.06(d,J=8.2Hz,1H),2.97(dd,J=10.2,6.4Hz,1H),2.88(s,1H),2.53 (dd,J=11.8,4.8,Hz,2H),2.50-2.45(m,2H),2.45-2.42(m,1H),2.39(s,1H) ),2.29(d,J=3.8Hz,2H),2.27(s,1H),2.08(d,J=6.6Hz,1H),1.94-1.88(m,2 H),1.88-1.83(m,1H),1.63(dd,J=4.8,1.8Hz,1H),1.59(dd,J=6.0,3.4Hz, 1H),1.39(s,1H),1.27(s,1H),1.16(t,J=7.0Hz,3H),1.06(t,J=7.0Hz,3H). 1313C NMR (100 MHz, CDCl3) δ 85.61, 84.05, 83.05, 80.30, 78.83, 78.62, 76.77, 62.23, 59.17, 59.06, 58.73, 56.56, 56.43, 53.61, 50.49, 49.64, 49.25, 49.09, 49.00, 41.57, 39.29, 36.63, 35.61, 35.49, 26.32, 16.12, 13.68.

[0044] Example 5: Preparation of Compound 5 Weighed 100 mg of Compound 4 and placed it in a 5 mL round-bottom flask, added 2 mL of dry pyridine to dissolve it, added 2-fold equivalent of cyclohexanecarbonyl chloride under Ar gas protection in an ice bath, reacted at room temperature (about 20 °C), detected the progress of the reaction by thin-layer chromatography, and after about 12 h, the reaction was complete. The reaction solution was rotary evaporated and separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [Chemical formula] Molecular formula C 41 H 65 NO9, light yellow foamy solid (122 mg), yield 85.0%.

[0045] HRESIMS m / z: [(M + H) + , 716.47] 1H NMR (400MHz, CDCl3) δ4.93(d,J=5.2Hz,1H),3.98(dd,J=6.6,1.6Hz,1H),3.85(t,J=7.8Hz,1H ),3.63(d,J=8.2Hz,1H),3.52-3.44(m,1H),3.40-3.32(m,1H),3.29(s,6H),3.25(s,3H),3.2 0(s,3H),3.05(d,J=8.2Hz,1H),2.98(dd,J=9.2,6.2Hz,1H),2.78(s,1H),2.52(dd,J=10.6,1 .6Hz,1H),2.48-2.44(m,1H),2.43(d,J=4.8Hz,1H),2.38(d,J=6.2Hz,3H),2.35-2.30(m,1H), 2.28(d,J=3.6Hz,1H),2.25(t,J=3.6Hz,1H),2.22(d,J=3.0Hz,1H),2.20(d,J=2.2Hz,1H),2. 05(d,J=6.4Hz,1H),1.99-1.91(m,3H),1.86(s,2H),1.83(d,J=3.2Hz,2H),1.70(t,J=8.2,3. 8Hz,5H),1.61(t,J=5.6Hz,3H),1.50-1.44(m,2H),1.42(s,1H),1.41-1.38(m,1H),1.32(s,1 H),1.28(s,2H),1.25-1.22(m,3H),1.21(s,1H),1.10(t,J=7.4Hz,3H),1.06(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ175.85,175.26,84.86,83.55,81.96,80.30,80.19,78.3 0,76.67,60.38,59.16,58.81,57.88,56.10,56.07,54.38,50.91,48.75,48.57 ,47.63,45.19,43.24,42.34,39.02,37.44,36.25,34.75,31.57,30.32,29.16,29.08,28.93,28.82,26.37,26.08,26.05,25.62,25.53,25.49,16.14,13.54.

[0046] Example 6: Preparation of compound 6 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of froyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the reaction was complete. The reaction mixture was evaporated by rotation, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 37 H 49 NO 11 Pale yellow foamy solid (137 mg), yield 90.0%. HRESIMS m / z:[(M+H)+,684.34] 1 H NMR(400MHz,CDCl3)δ7.57(dd,J=1.8,0.8Hz,1H),7.52(dd,J=1.8,0.8Hz,1H),7.19( dd,J=3.4,0.8Hz,1H),7.10(dd,J=3.4,0.8Hz,1H),6.48(dd,J=3.4,1.6Hz,1H),6.43( dd,J=3.4,1.6Hz,1H),5.20(d,J=5.2Hz,1H),4.15-4.06(m,1H),4.01(d,J=5.8Hz,1H) ,3.63(d,J=8.2Hz,1H),3.50(d,J=9.6Hz,1H),3.44-3.35(m,2H),3.35(s,3H),3.29(s ,4H),3.27(s,5H),3.23(s,4H),3.08(d,J=8.2Hz,1H),3.01(dd,J=9.8,6.2Hz,1H),2. 86(s,1H),2.65(t,J=6.2Hz,1H),2.55-2.43(m,4H),2.40(s,2H),2.37(d,J=6.6Hz,2H ),2.31(dd,J=14.2,8.8Hz,2H),2.11-2.02(m,3H),1.90(dd,J=12.2,6.0Hz,1H),1.74 (s,1H),1.68-1.58(m,2H),1.25(s,1H),1.10(t,J=7.2Hz,3H),0.69(t,J=6.8Hz,3H). 13C NMR(100MHz,CDCl3)δ158.79,157.92,146.28,146.17,145.27,145.03,11 8.23,118.11,111.80,111.80,85.12,83.61,83.34,80.76,80.27,78.19,7 7.79,61.24,59.16,58.86,58.22,56.25,56.04,53.89,50.83,49.08,49. 01,48.29,45.05,42.07,39.14,37.47,36.20,35.11,26.50,15.28,13.64.

[0047] Example 7: Preparation of Compound 7 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of 2-chloropropionyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the reaction was complete. The reaction mixture was evaporated by rotation, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 33 H 51 Cl2NO9, pale yellow foamy solid (98 mg), yield 71.9%. HRESIMS m / z:[(M+H)+,676.31] 1H NMR (400MHz, CDCl3) δ4.46-4.37(m,2H),4.30(t,J=6.6Hz,3H),4.07-4.02( m,1H),3.85(d,J=7.8Hz,1H),3.62(d,J=8.2Hz,1H),3.51-3.45(m,1H),3.4 0(t,J=7.4Hz,1H),3.32(s,3H),3.30(s,6H),3.27(s,3H),3.18(s,1H),2.9 9(t,J=6.6Hz,2H),2.89-2.81(m,1H),2.52-2.47(m,1H),2.45(d,J=4.6Hz,1 H),2.33-2.26(m,2H),2.15-2.11(m,1H),2.03(q,J=7.2Hz,2H),1.72(d,J= 2.8Hz,2H),1.70(d,J=7.4Hz,3H),1.66(dd,J=7.0,1.8Hz,2H),1.55(dd,J=8 .2,3.6Hz,1H),1.45(d,J=7.6Hz,1H),1.42(q,J=1.4Hz,1H),1.40(d,J=1.8 Hz,1H),1.13(t,J=6.2Hz,3H),1.09(d,J=7.4Hz,3H),0.95(t,J=7.4Hz,1H). 13 C NMR (100MHz, CDCl3) δ169.54,167.87,83.28,82.77,82.30,81.19,79.65,78.91,78.23,60.42,59.21,59.01,57.99,56.62,56.09 ,52.82,51.02,49.18,48.81,44.19,41.36,38.95,38.83,38.60,37.21,36.76,36.64,34.86,26.85,22.81,22.81,15.91,14.25.

[0048] Example 8: Preparation of compound 8 100 mg of compound 4 was weighed and placed in a 25 mL round-bottom flask. 5 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of cyclopropionyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the reaction was complete. The reaction mixture was evaporated by rotation, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 35 H 53 NO9, pale yellow foamy solid (102 mg), yield 79.9%. HRESIMS m / z:[(M+H) + ,632.38] 1 H NMR(400MHz,CDCl3)δ4.87(d,J=5.2Hz,1H),3.98(dd,J=6.6,1.6Hz,1H),3.87(t,J=8.2Hz,1H),3.61(d,J=8.2Hz,1H),3.47(dd,J=8.4,7.0Hz,1H), 3.36(dd,J=8.4,6.8Hz,1H),3.30(s,3H),3.28(s,3H),3.28(s,3H),3.19 (s,3H),3.05(d,J=8.2Hz,1H),2.98(dd,J=9.2,6.0Hz,1H),2.78(s,1H),2 .55-2.42(m,5H),2.36(d,J=1.6Hz,1H),2.23(dd,J=7.8,1.7Hz,3H),2.0 4(d,J=6.6Hz,1H),1.95-1.79(m,3H),1.69-1.65(m,1H),1.64-1.57(m,3H ),1.40(d,J=6.4Hz,1H),1.13(t,J=6.8Hz,3H),1.06(t,J=7.2Hz,3H),0. 88-0.84(m,2H),0.84-0.82(m,2H),0.82-0.80(m,2H),0.80-0.75(m,2H). 13C NMR(100MHz,CDCl3)δ174.87,174.02,84.63,83.22,82.11,80.44,80.04,78.06,77.20,65.57,60.43,59.03,58.72,58.04,56.06,55. 95,54.22,50.68,48.69,44.74,41.86,38.88,37.46,36.12,26.10,22.69,19.18,15.98,13.37,13.29,13.17,8.72,8.66,8.63,8.52.

[0049] Example 9: Preparation of Compound 9 100 mg of breiaconitine A was weighed and placed in a 25 mL round-bottom flask. 5 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-methoxybenzyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the reaction was complete. The reaction mixture was evaporated by rotation, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 43 H 55 NO 12 Pale yellow foamy solid (91 mg), yield 75.5%. HRESIMS m / z:[(M+H) + ,778.39] 1H NMR (400MHz, CDCl3) δ8.07(d,J=8.8Hz,2H),7.94(d,J=8.8Hz,2H),6.91(d,J=8.8Hz,2H),6.84(d,J=8.8Hz,2H),5.29-5.25(m,1H),4.14(dd,J=8.8,5 .6Hz,1H),3.99(d,J=6.6Hz,1H),3.84(s,3H),3.81(s,3H),3.62(d,J=8.4H z,1H),3.52(d,J=10.4Hz,1H),3.32(s,3H),3.28(s,3H),3.25(s,3H),3.16 (s,3H),3.03(s,3H),2.88(t,J=6.2Hz,1H),2.58(dd,J=12.2,7.2Hz,1H), 2.55-2.51(m,1H),2.49(d,J=5.8Hz,1H),2.47(s,1H),2.37-2.21(m,1H),2 .15-2.05(m,3H),1.92(t,J=9.2Hz,1H),1.65-1.57(m,2H),1.41(d,J=5.4H z,1H),1.35(s,3H),1.28(s,1H),1.21-1.15(m,1H),1.10(t,J=7.2Hz,3H). 13 C NMR (100MHz, CDCl3) δ169.97,166.37,165.50,163.60,163.28,132.10,132.10,131.9 4,131.94,123.38,122.74,113.88,113.88,113.54,113.54,85.69,84.81,83.40,82.5 6,80.53,80.53,77.28,61.53,59.22,58.40,57.94,56.12,55.56,55.49,53.99,50.43,49.32,49.09,44.05,41.96,39.82,39.22,35.79,35.02,29.81,26.38,21.85,13.59.

[0050] Example 10: Preparation of Compound 10 100 mg of breiaconitine A was weighed and placed in a 25 mL round-bottom flask. 5 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of cyclopropyl carbonyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the reaction was complete. The reaction mixture was evaporated by rotation, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 39 H 53 NO 11 Pale yellow foamy solid (80 mg), yield 73.1%. HRESIMS m / z:[(M+H)+,712.38] 1 H NMR(400MHz,CDCl3)δ8.07(d,J=8.8Hz,2H),6.93(d,J=8.8Hz,2H),5.12(d,J=5.2Hz,1H),4.02-3.96(m,2H),3.87(s,3H),3.62(d,J= 8.4Hz,1H),3.37(s,3H),3.29(s,3H),3.24(s,3H),3.16(s,3H),3.02(d,J=11.8Hz,3H),2.98(s,1H),2.85(t,J=6.2Hz,1H),2.59-2. 53(m,1H),2.52-2.49(m,1H),2.46(d,J=6.0Hz,2H),2.35-2.25(m,1H),2.12-2.06(m,2H),2.03-1.97(m,1H),1.95(s,1H),1.65-1.6 2(m,1H),1.61-1.57(m,1H),1.42(s,1H),1.32(s,3H),1.30(s,1H),1.27(s,2H),1.09(t,J=7.2Hz,3H),0.96(dd,J=4.4,2.8Hz,2H). 13C NMR(100MHz, CDCl3)δ173.94,169.84,166.16,163.46,131.97,131.97,122. 64,113.74,113.74,85.53,84.62,83.24,82.02,80.38,80.29,77.02,61.34, 59.10, 58.30, 57.80, 55.89, 55.44, 53.86, 50.25, 49.14, 48.93, 48.90, 43.82, 41.71, 39.64, 39.07, 35.58, 34.85, 26.24, 21.68, 13.42, 13.23, 8.53, 8.47.

[0051] Example 11: Preparation of Compound 11 100 mg of breiaconitine A was weighed and placed in a 25 mL round-bottom flask. 5 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of cyclohexanecarbonyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the reaction was complete. The reaction mixture was evaporated by rotation, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 42 H 59 NO 11 Pale yellow foamy solid (76 mg), yield 65.1%. HRESIMS m / z:[(M+H)+,754.43] 1H NMR (400MHz, CDCl3) δ8.04(d,J=8.8Hz,2H),6.92(d,J=8.8Hz,2H),5.06(d,J=5.2Hz,1H),3.97(dd,J=9.8,6.2Hz,2H),3.85(s,3H),3.61(d,J= 8.4Hz,1H),3.39(dd,J=15.6,5.8Hz,1H),3.33(s,3H),3.27(s,3H),3.23(s,3H),3.14(s,3H),3.03-2.93(m,4H),2.83(dd,J=7.4,5.4Hz,1H),2 .58-2.48(m,2H),2.46-2.39(m,3H),2.27(ddt,J=11.2,7.2,3.6Hz,2H),2.11-2.02(m,2H),1.95-1.86(m,3H),1.84(d,J=2.4Hz,1H),1.70(dd ,J=9.6,3.6Hz,2H),1.63-1.55(m,3H),1.46-1.35(m,3H),1.31(s,3H), 1.28(d,J=2.8Hz,1H),1.21(s,1H),1.16(s,1H),1.08(t,J=7.2Hz,3H). 13 C NMR (100MHz, CDCl3) δ175.39,169.96,166.26,163.56,132.05,132.05,122.86,11 3.87,113.87,85.74,84.69,83.39,81.74,80.53,80.15,77.18,61.40,59.23,58.2 2,57.92,55.99,55.57,54.03,50.38,49.28,49.02,48.99,43.86,43.20,41.95,39.72,39.19,35.68,34.97,29.22,29.07,26.39,25.94,25.54,25.47,21.82,13.56.

[0052] Example 12: Preparation of Compound 12 100 mg of breiaconitine A was weighed and placed in a 25 mL round-bottom flask. 5 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of froyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the reaction was complete. The reaction mixture was evaporated by rotation, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 40 H 51 NO 12 Pale yellow foamy solid (72 mg), yield 63.5%. HRESIMS m / z:[(M+H)+,738.36] 1 H NMR(400MHz,CDCl3)δ8.05(d,J=8.8Hz,2H),7.52(dd,J=1.6,0.8Hz,1H),7.08( dd,J=3.4,0.8Hz,1H),6.91(d,J=8.8Hz,2H),6.43(dd,J=3.4,1.6Hz,1H),5.23 (d,J=5.2Hz,1H),4.12(dd,J=9.0,5.8Hz,1H),3.98(d,J=6.6Hz,1H),3.84(s,3 H),3.62(d,J=8.4Hz,1H),3.55-3.49(m,1H),3.36(s,3H),3.27(s,3H),3.24(s ,3H),3.15(s,3H),3.07-2.97(m,4H),2.92-2.86(m,1H),2.59(dd,J=12.2,7.2 Hz,1H),2.53(d,J=5.8Hz,1H),2.49(d,J=5.8Hz,2H),2.47-2.43(m,1H),2.33- 2.25(m,1H),2.14-2.08(m,2H),2.07(s,1H),1.97-1.89(m,1H),1.65-1.61(m, 1H),1.61-1.54(m,1H),1.33(s,3H),1.20-1.14(m,1H),1.10(t,J=7.2Hz,3H). 13C NMR(100MHz,CDCl3)δ169.95,166.29,163.62,157.88,146.24,144.95,132.09, 132.09,122.66,118.08,113.89,113.89,111.80,85.56,84.83,83.38,83.24,80 .55,80.51,77.12,61.94,59.23,58.44,57.94,56.16,55.57,53.75,50.39,49.40,49.27,49.09,43.99,41.85,39.78,39.24,35.65,35.09,26.43,21.81,13.62.

[0053] Example 13: Preparation of Compound 13 100 mg of compound 4 was weighed and placed in a 25 mL round-bottom flask. 5 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-methoxybenzyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the reaction was complete. The reaction mixture was evaporated by rotation, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 43 H 57 NO 11 Pale yellow foamy solid (118 mg), yield 76.4%. HRESIMS m / z:[(M+H)+,764.41] 1H NMR(400MHz, CDCl3)δ8.09(d,J=8.8Hz,2H),7.95(d,J=9.0Hz,2H),6.91(d,J= 8.8Hz,2H),6.85(d,J=9.0Hz,2H),5.24(d,J=5.2Hz,1H),4.17-4.11(m,1H),4. 04(d,J=7.4Hz,1H),3.85(s,3H),3.81(s,3H),3.63(d,J=8.2Hz,1H),3.49-3.4 4(m,1H),3.41-3.35(m,1H),3.32(s,3H),3.30(s,3H),3.27(s,3H),3.24(s,3H ),3.23-3.18(m,1H),3.10(d,J=8.2Hz,1H),3.03(dd,J=9.6,6.2Hz,1H),2.91 (s,1H),2.66(t,J=5.4Hz,1H),2.53(t,J=9.6Hz,2H),2.46(d,J=11.2Hz,2H),2 .41-2.33(m,3H),2.09(d,J=8.4Hz,3H),1.89(dd,J=11.8,5.8Hz,1H),1.64(q, J=5.4Hz,2H),1.22-1.15(m,1H),1.11(t,J=7.2Hz,3H),0.64(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ166.51,165.61,163.27,163.21,132.14,132.14,131.96,131.9 6,123.61,123.48,113.55,113.55,113.53,113.53,85.18,83.35,83.16,80.78,80.34 ,78.18,77.68,60.90,59.19,58.86,58.24,56.25,56.02,55.51,55.51,54.20,50.90,49.08,48.94,48.23,45.28,42.37,39.17,37.69,36.36,35.03,26.45,15.49,13.65.

[0054] Example 14: Preparation of Compound 14 100 mg of compound 2 was weighed and placed in a 25 mL round-bottom flask. 5 ml of dried pyridine was added to dissolve it, and under Ar gas protection, 2 equivalents of cyclohexanecarbonyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the reaction was complete. The reaction mixture was evaporated by rotation, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 42 H 61 NO 10 Pale yellow foamy solid (101 mg), yield 85.8%. HRESIMS m / z:[(M+H)+,740.45] 1H NMR (400MHz, CDCl3) δ8.05(d,J=8.8Hz,2H),6.91(d,J=8.8Hz,2H),5.03(d,J=5.2Hz,1H),3 .98(dd,J=12.2,6.2Hz,2H),3.85(s,3H),3.61(d,J=8.2Hz,1H),3.36(s,1H),3.33(s,3H),3 .31(s,1H),3.29(s,3H),3.25(s,3H),3.22(s,3H),3.17-3.10(m,1H),3.08(d,J=8.2Hz,1H ),3.00(dd,J=9.4,6.2Hz,1H),2.83(s,1H),2.64-2.59(m,1H),2.51(t,J=8.8Hz,2H),2.48- 2.41(m,2H),2.35-2.33(m,1H),2.31-2.26(m,3H),2.06(d,J=6.4Hz,1H),2.04-1.98(m,1H ),1.90-1.86(m,2H),1.86-1.83(m,2H),1.69(dd,J=9.6,3.6Hz,2H),1.62(dd,J=6.6,4.8Hz ,2H),1.59-1.54(m,1H),1.41(d,J=4.6Hz,1H),1.40-1.37(m,1H),1.33(s,1H),1.28(d,J=2 .6Hz,2H),1.25(s,1H),1.20(d,J=7.8Hz,2H),1.07(t,J=7.2Hz,3H),0.57(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ175.49,166.38,163.20,132.05,132.05,123.57,113.52,11 3.52,85.04,83.32,82.30,80.44,80.33,78.15,77.59,60.73,59.17,58.82,58.06 ,56.09,55.94,55.50,54.25,50.83,48.96,48.84,48.13,45.03,43.21,42.32,39.11,37.56,36.22,34.93,29.24,29.06,26.43,25.97,25.56,25.47,15.42,13.59.

[0055] Example 15: Preparation of Compound 15 100 mg of compound 2 was weighed and placed in a 25 mL round-bottom flask. 5 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of froyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the reaction was complete. The reaction mixture was evaporated by rotation, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 40 H 53 NO 11 Pale yellow foamy solid (102 mg), yield 89%. HRESIMS m / z:[(M+H)+,724.38] 1 H NMR(400MHz,CDCl3)δ8.06(d,J=8.8Hz,2H),7.51(dd,J=1.8,0.8Hz,1H),7.08(d d,J=3.5,0.8Hz,1H),6.90(d,J=8.8Hz,2H),6.42(dd,J=3.4,1.6Hz,1H),5.20(d ,J=5.2Hz,1H),4.15-4.09(m,1H),4.04-4.00(m,1H),3.85(s,3H),3.63(d,J=8. 2Hz,1H),3.48-3.44(m,1H),3.36(s,3H),3.29(s,3H),3.26(s,3H),3.23(s,3H), 3.18(d,J=14.8Hz,1H),3.09(d,J=8.2Hz,1H),3.02(dd,J=9.8,6.2Hz,1H),2.88 (s,1H),2.67(dt,J=6.2,3.0Hz,1H),2.52(dd,J=13.2,7.2Hz,3H),2.38(d,J=4.0 Hz,2H),2.37-2.32(m,2H),2.08(d,J=5.2Hz,3H),1.95-1.86(m,1H),1.64(q,J= 4.8Hz,2H),1.26(d,J=11.2Hz,2H),1.10(t,J=7.2Hz,3H),0.61(t,J=6.8Hz,3H). 13C NMR(100MHz,CDCl3)δ166.42,163.27,158.00,146.14,145.12,132.11,132.11, 123.36,117.98,113.55,113.55,111.78,85.20,83.82,83.28,80.79,80.29,78. 08,77.36,61.34,59.17,58.86,58.27,56.28,56.01,55.50,53.92,50.85,49.10,48.31,45.18,42.22,39.17,37.60,36.20,35.11,29.82,26.47,15.41,13.64.

[0056] Example 16: Preparation of Compound 16 100 mg of compound 2 was weighed and placed in a 25 mL round-bottom flask. 5 ml of dried pyridine was added to dissolve it, and under Ar gas protection, 2 equivalents of cyclopropane carbonyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the reaction was complete. The reaction mixture was evaporated by rotation, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 39 H 55 NO 10 Pale yellow foamy solid (103 mg), yield 93.5%. HRESIMS m / z:[(M+H)+,698.40] 1H NMR (400MHz, CDCl3) δ8.05(d,J=8.8Hz,2H),6.91(d,J=8.8Hz,2H),5.06(d,J=5.2Hz,1 H),4.03-3.93(m,2H),3.85(s,3H),3.61(d,J=8.2Hz,1H),3.36(s,3H),3.32(dd,J=6. 4,1.6Hz,1H),3.28(s,3H),3.24(s,3H),3.21(s,3H),3.18-3.12(m,1H),3.08(d,J=8. 2Hz,1H),3.00(dd,J=9.6,6.2Hz,1H),2.82(s,1H),2.61(t,J=6.2Hz,1H),2.54-2.47( m,2H),2.48-2.40(m,2H),2.36-2.31(m,2H),2.30(d,J=3.8Hz,1H),2.27(d,J=5.4Hz, 1H),2.08-2.04(m,1H),2.01(d,J=5.6Hz,1H),1.99-1.91(m,1H),1.87(dd,J=12.0,5. 8Hz,1H),1.62(dd,J=6.8,4.8Hz,2H),1.57(dt,J=8.0,4.6Hz,1H),1.25(s,1H),1.07( t,J=7.2Hz,3H),0.96-0.91(m,2H),0.77(dd,J=8.2,2.8Hz,2H),0.57(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ174.13,166.40,163.23,132.10,132.10,123.48,113. 51,113.51,85.10,83.29,82.70,80.69,80.31,78.10,77.53,60.82,59.16,5 8.82,58.26,56.12,55.95,55.50,54.18,50.82,48.98,48.88,48.17,45.12,42.21,39.12,37.59,36.25,34.97,26.43,15.38,13.60,13.43,8.56,8.52.

[0057] Example 17: Preparation of Compound 17 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of tenoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 37 H 49 NO9S2, pale yellow solid (65.4 mg), yield 45.7%. HRESIMS m / z:[(M+H) + ,716.28] 1 H NMR(400MHz,Chloroform-d)δ7.84(dd,J=3.6,1.2Hz,1H),7.74(dd,J=3.6,1.2Hz,1H),7 .53(dd,J=5.0,1.2Hz,1H),7.48(dd,J=5.0,1.2Hz,1H),7.08(dd,J=5.0,3.6Hz,1H),7.0 3(dd,J=5.0,3.6Hz,1H),5.23(d,J=5.2Hz,1H),4.09(dd,J=8.8,6.4Hz,1H),4.02(dd,J= 6.6,1.4Hz,1H),3.65(d,J=8.2Hz,1H),3.41(dd,J=13.2,4.8Hz,2H),3.33(s,3H),3.30( s,3H),3.28(s,3H),3.24(s,3H),3.08(d,J=8.2Hz,1H),3.02(dd,J=9.6,6.2Hz,1H),2.8 7(s,1H),2.64(t,J=6.2Hz,1H),2.56-2.50(m,2H),2.46(d,J=11.8Hz,2H),2.43-2.39(m ,2H),2.31(dd,J=14.2,8.8Hz,2H),2.10(d,J=6.0Hz,3H),1.90(dd,J=12.2,6.0Hz,1H), 1.74(s,2H),1.65(dd,J=13.0,4.6Hz,2H),1.10(t,J=7.2Hz,3H),0.69(t,J=6.8Hz,3H). 13 C NMR(100MHz,CDCl3)δ162.24,161.46,134.70,134.62,133.69,133.55,13 2.40,132.18,127.70,127.70,85.12,83.77,83.30,80.55,80.27,78.18,7 7.84,60.89,59.17,58.86,58.05,56.27,56.10,54.10,50.84,48.94,48. 89,48.09,45.22,42.20,39.11,37.50,36.12,35.02,26.43,15.30,13.61.

[0058] Example 18: Preparation of Compound 18 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of 5-chlorothiophene-2-carbonyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 37 H 47 Cl2NO9S2, pale yellow solid (87.4 mg), yield 55.8%. HRESIMS m / z:[(M+H) + ,784.20] 1H NMR(400MHz,Chloroform-d)δ7.63(d,J=4.0Hz,1H),7.52(d,J=4.0Hz,1H),6.92(d,J=4.0Hz,1H),6.87(d,J=4.0Hz,1H),5.17(d,J=5.2Hz,1H) ,4.08-3.97(m,2H),3.65(d,J=8.2Hz,1H),3.49-3.37(m,2H),3.31(s, 3H),3.30(s,3H),3.28(s,3H),3.23(s,3H),3.06(d,J=8.2Hz,1H),3.01 (dd,J=9.8,6.2Hz,1H),2.84(s,1H),2.60(t,J=5.8Hz,1H),2.50(s,2H),2.48(s,2H),2.41(s,1H),2.32(d,J=6.8Hz,2H),2.08(dd,J=11.6,6. 8Hz,3H),1.90(dd,J=11.8,5.8Hz,1H),1.76(s,2H),1.66(d,J=4.2Hz,1H),1.61(d,J=5.8Hz,1H),1.09(t,J=7.2Hz,3H),0.78(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ161.10,160.37,137.38,137.11,133.24,133.11,13 2.69,132.58,127.28,127.24,85.14,84.05,83.23,80.28,80.23,78.12,7 7.90,61.03,59.17,58.91,58.04,56.25,56.18,53.98,50.82,49.00,48. 96,48.13,45.20,42.13,39.12,37.52,35.98,35.10,26.42,15.51,13.62.

[0059] Example 19: Preparation of Compound 19 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of tenoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 40 H 53 NO 10 S, pale yellow solid (80.4 mg), yield 68.5%. HRESIMS m / z:[(M+H) + ,740.33] 1 H NMR(400MHz,Chloroform-d)δ8.08(d,J=8.8Hz,2H),7.73(dd,J=3.8,1.2Hz,1H),7.4 7(dd,J=4.8,1.2Hz,1H),7.02(dd,J=5.0,3.6Hz,1H),6.91(d,J=8.8Hz,2H),5.22(d, J=5.2Hz,1H),4.14-4.09(m,1H),4.03(d,J=6.4Hz,1H),3.85(s,3H),3.63(d,J=8.2H) z,1H),3.44(d,J=9.8Hz,1H),3.38(d,J=8.6Hz,1H),3.35(s,3H),3.30(s,3H),3.27(s ,3H),3.24(s,3H),3.21-3.16(m,1H),3.09(d,J=8.2Hz,1H),3.03(dd,J=9.8,6.2Hz, 1H),2.88(s,1H),2.66(t,J=6.4Hz,1H),2.53(t,J=8.4Hz,2H),2.49-2.43(m,2H),2. 40-2.33(m,3H),2.11(d,J=8.8Hz,2H),1.90(dd,J=11.6,5.8Hz,1H),1.70(s,1H),1. 64(dd,J=11.6,5.8Hz,2H),1.28(s,1H),1.10(t,J=7.2Hz,3H),0.63(t,J=6.8Hz,3H). 13 C NMR(100MHz,CDCl3)δ166.45,163.27,161.52,134.84,133.47,132.11,132.11, 127.66,123.42,113.56,113.56,113.56,85.16,83.88,83.32,80.82,80.32,78. 13, 77.36, 60.96, 59.18, 58.86, 58.29, 56.25, 56.03, 55.50, 54.13, 50.86, 49.05, 48.95, 48.24, 45.20, 42.31, 39.16, 37.65, 36.17, 35.04, 26.46, 15.46, 13.63.

[0060] Example 20: Preparation of Compound 20 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of 5-chlorothiophene-2-carbonyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 40 H 52 ClNO 10 S, pale yellow solid (82.8 mg), yield 67.4%. HRESIMS m / z:[(M+H) + ,774.30] 1H NMR(400MHz,Chloroform-d)δ8.07(d,J=8.8Hz,2H),7.51(d,J=4.0Hz,1H),6.91(d,J=8.8Hz,2H),6.85(d,J=4.0Hz,1H),5.19(d,J=5.2Hz,1H),4.0 9-4.00(m,2H),3.86(s,3H),3.64(d,J=8.2Hz,1H),3.45-3.40(m,1H),3. 40-3.35(m,1H),3.34(s,3H),3.30(s,3H),3.27(s,3H),3.24(s,3H),3.22 -3.16(m,1H),3.09(d,J=8.2Hz,1H),3.03(dd,J=9.8,6.2Hz,1H),2.86(s ,1H),2.65(t,J=5.6Hz,1H),2.57-2.49(m,2H),2.49-2.42(m,2H),2.35(d d,J=14.8,8.2Hz,3H),2.09(d,J=6.6Hz,3H),1.91(dd,J=12.2,6.2Hz,1H ),1.63(s,3H),1.28(s,1H),1.10(t,J=7.2Hz,3H),0.64(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ166.37,163.32,160.48,136.99,133.01,132.96,132.09, 132.09,127.20,123.35,113.59,113.59,85.18,84.21,83.30,80.66,80.31,78. 10,77.36,61.03,59.18,58.87,58.22,56.24,56.06,55.52,54.08,50.86,49.07,48.98,48.27,45.21,42.27,39.17,37.62,36.13,35.08,26.47,15.48,13.65.

[0061] Example 21: Preparation of Compound 21 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of tenoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was evaporated by rotation, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 40 H 51 NO 11 S, pale yellow solid (63.4 mg), yield 54.3%. HRESIMS m / z:[(M+H) + ,754.31] 1 H NMR(400MHz,Chloroform-d)δ8.06(d,J=8.8Hz,2H),7.72(dd,J=3.6,1.2Hz,1H),7.47(dd,J=5.0,1.2Hz,1H),7.0 2(dd,J=5.0,3.6Hz,1H),6.90(d,J=8.8Hz,2H),5.24(d,J=5.2Hz,1H),4.10(dd,J=8.8,5.8Hz,1H),3.98(d,J=6.6 40Hz,1H),3.84(s,3H),3.62(d,J=8.4Hz,1H),3.55-3.43(m,1H),3.35(s,3H),3.27(s,3H),3.24(s,3H) ,3.15(s,3H),3.08-3.03(m,1H),3.01(d,J=6.0Hz,3H),2.89(t,J=6.4Hz,1H),2.58(dd,J=12.2,7.2Hz,1 H),2.51(dd,J=10.0,5.8Hz,2H),2.45(dd,J=14.8,4.2Hz,2H),2.35-2.23(m,1H),2.12(dd,J=11.2,5.8H z,3H),1.96-1.89(m,1H),1.61(dd,J=12.8,3.8Hz,2H),1.34(s,3H),1.27(s,1H),1.09(t,J=7.2Hz,3H). 13C NMR(100MHz,CDCl3)δ169.93,166.29,163.59,161.36,134.53,133.53,132.22, 132.06,132.06,127.66,122.67,113.87,113.87,85.57,84.76,83.36,83.26,80 .55,80.48,77.09,61.58,59.20,58.43,57.92,56.10,55.54,53.90,50.38,49.32,49.10,49.03,43.98,41.89,39.77,39.20,35.60,35.01,26.37,21.81,13.56.

[0062] Example 22: Preparation of Compound 22 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of 5-chlorothiophene-2-carbonyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 40 H 50 ClNO 11 S, pale yellow solid (92.5 mg), yield 75.8%. HRESIMS m / z:[(M+H) + ,788.27] 1H NMR(400MHz,Chloroform-d)δ8.04(d,J=8.8Hz,2H),7.51(d,J=4.0Hz,1H),6.91(d,J=8.8Hz,2H),6.85(d,J=4.0Hz,1H),5.21(d,J=5.2 Hz,1H),4.05(dd,J=8.8,5.8Hz,1H),3.98(d,J=6.6Hz,1H),3.84(s,3H),3.62(d,J=8.4Hz,1H),3.52-3.45(m,1H),3.33(s,3H),3.27(s, 3H),3.24(s,3H),3.15(s,3H),3.04(d,J=8.6Hz,1H),3.00(d,J=12.4Hz,3H),2.90-2.85(m,1H),2.57(dd,J=12.2,7.2Hz,1H),2.53-2. 40(m,4H),2.35-2.23(m,1H),2.17-2.05(m,3H),1.98-1.88(m,1H),1.80(s,1H),1.69-1.54(m,2H),1.35(s,3H),1.09(t,J=7.2Hz,3H). 13 C NMR (100MHz, CDCl3) δ169.93,166.21,163.63,160.31,137.10,133.08,132.63, 132.04,132.04,127.20,122.59,113.90,113.90,85.51,84.77,83.57,83.35,80 .47,80.40,76.95,61.63,59.21,58.37,57.94,56.09,55.55,53.86,50.37,49.34,49.12,49.03,43.96,41.85,39.73,39.21,35.54,35.04,26.39,21.82,13.57.

[0063] Example 23: Preparation of Compound 23 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of tetrahydropyrancarbonyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 39 H 61 NO 11 Pale yellow solid (67.3 mg), yield 46.8%. HRESIMS m / z:[(M+H) + ,720.42] 1 H NMR(400MHz,Chloroform-d)δ4.96(d,J=5.2Hz,1H),3.97(d,J=5.8Hz,2H),3.95-3.89 (m,3H),3.86(t,J=7.6Hz,1H),3.64(d,J=8.2Hz,1H),3.53-3.47(m,1H),3.47(d,J=2.8 Hz,1H),3.45-3.40(m,3H),3.40-3.32(m,2H),3.29(s,3H),3.29(s,3H),3.23(s,3H),3 .20(s,3H),3.03(d,J=8.2Hz,1H),2.98(dd,J=9.4,6.2Hz,1H),2.77(s,1H),2.54(dd,J =9.6,5.2Hz,2H),2.48(dt,J=11.2,4.2Hz,3H),2.43(s,1H),2.40(d,J=4.6Hz,2H),2. 26(dd,J=13.8,8.6Hz,2H),2.16(dd,J=13.8,6.8Hz,1H),2.07(d,J=6.4Hz,1H),1.97(d d,J=12.8,5.8Hz,1H),1.90(s,1H),1.84(dd,J=8.6,4.4Hz,3H),1.78(d,J=4.2Hz,3H), 1.74(d,J=3.4Hz,3H),1.68-1.57(m,2H),1.11(t,J=6.8Hz,3H),1.06(t,J=7.2Hz,3H). 13 C NMR(100MHz,CDCl3)δ174.13,173.58,84.92,83.39,82.48,80.20,79.82,7 8.27,67.32,67.25,67.20,67.14,60.55,59.15,58.88,57.80,56.14,56.12 ,54.19,50.86,48.82,48.63,47.66,45.22,42.23,40.25,39.98,39.01,37.51,36.12,34.89,31.63,28.85,28.69,28.64,28.47,26.36,16.24,13.55.

[0064] Example 24: Preparation of Compound 24 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of tetrahydropyrancarbonyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 59 NO 11 Pale yellow solid (86.2 mg), yield 73.2%. HRESIMS m / z:[(M+H) + ,742.40] 1H NMR(400MHz,Chloroform-d)δ8.04(d,J=8.8Hz,2H),6.91(d,J=8.8Hz,2H),5.04(d,J=5.2Hz,1H ),3.98(q,J=7.0Hz,2H),3.92(t,J=3.8Hz,1H),3.90-3.87(m,1H),3.86(s,3H),3.62(d,J=8.2H z,1H),3.41(dd,J=3.4,1.8Hz,1H),3.38(d,J=3.6Hz,1H),3.37-3.34(m,1H),3.33(s,3H),3.29 (s,3H),3.26(s,3H),3.23(s,3H),3.18-3.12(m,1H),3.08(d,J=8.2Hz,1H),3.01(dd,J=9.6,6. 2Hz,1H),2.82(s,1H),2.64-2.59(m,1H),2.56-2.52(m,1H),2.51(s,1H),2.48(d,J=7.2Hz,1H) ,2.45(s,1H),2.43(d,J=3.0Hz,1H),2.35(s,1H),2.30(dd,J=7.8,4.2Hz,2H),2.07(d,J=6.6Hz ,1H),2.05-1.99(m,1H),1.97-1.91(m,1H),1.88(t,J=3.2Hz,1H),1.83-1.76(m,3H),1.74(dt, J=5.6,2.8Hz,1H),1.66(s,3H),1.63-1.60(m,1H),1.08(t,J=7.2Hz,3H),0.60(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ173.83,166.31,163.28,132.01,132.01,123.44,113.58,1 13.58,85.08,83.31,82.79,80.31,80.21,78.15,77.36,67.23,67.16,60.82,59 .18,58.85,57.90,56.11,56.01,55.52,54.18,50.85,49.01,48.89,48.18,45.04,42.31,40.00,39.13,37.53,36.15,34.99,28.86,28.80,26.44,15.47,13.61.

[0065] Example 25: Preparation of Compound 25 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of tetrahydropyrancarbonyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was evaporated by rotation, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 57 NO 12 Pale yellow solid (65.9 mg), yield 56.3%. HRESIMS m / z:[(M+H) + ,756.38] 1 H NMR(400MHz,Chloroform-d)δ8.02(d,J=8.8Hz,2H),6.91(d,J=8.8Hz,2H),5.06(d ,J=5.2Hz,1H),3.99-3.93(m,2H),3.93-3.87(m,2H),3.85(s,3H),3.61(d,J=8.4H z,1H),3.43(dd,J=7.8,4.8Hz,1H),3.40(d,J=2.2Hz,1H),3.37(d,J=3.6Hz,1H),3 .32(s,3H),3.27(s,3H),3.23(s,3H),3.14(s,3H),3.12(s,1H),2.98(d,J=6.2Hz, 2H),2.95(s,1H),2.83(dd,J=7.2,5.4Hz,1H),2.58-2.53(m,1H),2.53-2.50(m,1H) ),2.50(d,J=4.8Hz,1H),2.44(t,J=4.2Hz,2H),2.42-2.39(m,1H),2.34-2.22(m,1 H),2.13-2.03(m,2H),1.92(dd,J=15.6,12.2Hz,2H),1.84-1.79(m,1H),1.79-1.7 6(m,3H),1.75-1.71(m,1H),1.64-1.55(m,2H),1.33(s,3H),1.08(t,J=7.2Hz,3H). 13 C NMR(100MHz,CDCl3)δ173.70,169.93,166.16,163.61,131.98,122.70,113.90, 85.63,84.69,83.36,82.18,80.49,79.92,77.04,67.18,67.11,61.45,59.21,58 .06,57.93,55.98,55.56,53.96,50.37,49.29,49.04,48.99,43.83,41.91,40.02,39.65,39.18,35.59,34.99,31.55,30.31,28.83,28.76,26.38,21.81,13.55.

[0066] Example 26: Preparation of Compound 26 100 mg of compound 3 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of tetrahydropyrancarbonyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 38 H 59 NO 11 Pale yellow solid (123.2 mg), yield 83.2%. HRESIMS m / z:[(M+H) + ,706.40] 1H NMR(400MHz,Chloroform-d)δ4.91(d,J=5.2Hz,1H),3.97(t,J=3.8Hz,1H),3.93(d,J=3.6Hz,3H),3 .90(d,J=3.8Hz,1H),3.87(d,J=8.2Hz,1H),3.63(d,J=8.2Hz,1H),3.46(dd,J=4.8,2.4Hz,1H),3.45 -3.42(m,2H),3.42-3.37(m,2H),3.30(s,3H),3.29(s,3H),3.25(s,3H),3.20(s,3H),3.15(s,3H), 3.08(d,J=8.2Hz,1H),2.98(dd,J=9.4,6.2Hz,1H),2.78(s,1H),2.55(t,J=4.6Hz,1H),2.52(s,1H), 2.50-2.47(m,1H),2.46(d,J=4.4Hz,1H),2.44(d,J=2.4Hz,1H),2.43-2.41(m,1H),2.39(t,J=6.2H z,2H),2.29-2.24(m,1H),2.21(d,J=8.6Hz,1H),2.15(d,J=6.8Hz,1H),2.04(d,J=6.4Hz,1H),1.97( ddd,J=12.4,7.2,5.2Hz,1H),1.88(s,1H),1.84(q,J=2.8,2.0Hz,3H),1.81(d,J=3.6Hz,1H),1.78( d,J=2.8Hz,1H),1.76(t,J=5.2Hz,3H),1.74-1.70(m,1H),1.65-1.57(m,2H),1.07(t,J=7.2Hz,3H). 13 C NMR (100MHz, CDCl3) δ174.22,173.58,84.89,83.22,82.43,80.30,79.86, 78.45,77.03,67.30,67.27,67.19,67.15,60.68,59.17,58.85,57.82,56 .04,54.18,50.81,48.87,48.66,48.14,48.14,44.95,42.25,40.30,40.0 1,39.07,36.87,36.15,34.91,28.83,28.77,28.70,28.54,26.39,13.58.

[0067] Example 27: Preparation of Compound 27 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of nicotinoyl chloride hydrochloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 39 H 51 N3O9, pale yellow solid (102.3 mg), yield 72.5%. HRESIMS m / z:[(M+H) + ,706.36] 1H NMR(400MHz,Chloroform-d)δ9.31(d,J=1.2Hz,1H),9.16(d,J=1.2Hz,1H),8.75(dd,J=5.0,1 .8Hz,1H),8.70(dd,J=5.0,1.8Hz,1H),8.36(dt,J=7.8,2.0Hz,1H),8.22(dt,J=7.8,2.0Hz,1H ),7.38(ddd,J=8.0,4.8,0.8Hz,1H),7.31(ddd,J=8.0,4.8,0.8Hz,1H),5.32(d,J=5.2Hz,1H), 4.14(t,J=7.4Hz,1H),4.01(d,J=6.4Hz,1H),3.64(d,J=8.2Hz,1H),3.49(d,J=9.8Hz,1H),3.4 4-3.35(m,1H),3.29(s,6H),3.27(s,3H),3.24(s,3H),3.22-3.17(m,1H),3.04(dd,J=16.2,7. 2Hz,2H),2.89(s,1H),2.67(t,J=5.6Hz,1H),2.56-2.50(m,2H),2.47(d,J=4.8Hz,1H),2.45(s ,1H),2.41(s,1H),2.38(d,J=2.8Hz,1H),2.36(s,1H),2.14-2.08(m,3H),2.00-1.87(m,2H),1 .67(d,J=3.4Hz,1H),1.62(q,J=5.6,4.6Hz,1H),1.09(t,J=7.2Hz,3H),0.63(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ165.15,164.35,153.23,153.14,151.49,151.18,137.35 ,137.21,126.66,126.48,123.21,123.15,85.11,84.01,83.07,80.10,80.05, 78.06,77.81,61.06,59.03,58.83,58.02,56.08,56.02,53.81,50.74,49.08,48.93,48.22,45.20,42.12,39.06,37.54,36.01,35.12,26.33,15.45,13.54.

[0068] Example 28: Preparation of Compound 28 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of nicotinoyl chloride hydrochloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 54 N2O 10 Pale yellow solid (96.9 mg), yield 83.1%. HRESIMS m / z:[(M+H) + ,735.37] 1 H NMR(400MHz,Chloroform-d)δ9.17(d,J=1.6Hz,1H),8.71(dd,J=4.8,1.8Hz,1H),8. 24(dt,J=8.0,2.0Hz,1H),8.07(d,J=8.8Hz,2H),7.31(dd,J=8.0,4.8Hz,1H),6.91( d,J=9.0Hz,2H),5.26(d,J=5.2Hz,1H),4.12(t,J=7.6Hz,1H),4.04(d,J=6.6Hz,1H) ,3.85(s,3H),3.64(d,J=8.2Hz,1H),3.58-3.46(m,2H),3.39(p,J=7.2Hz,2H),3.31 (s,3H),3.30(s,3H),3.28(s,3H),3.25(s,3H),3.23-3.18(m,1H),3.09(d,J=8.2Hz ,1H),3.04(dd,J=9.8,6.2Hz,1H),2.89(s,1H),2.70-2.64(m,1H),2.53(t,J=3.6Hz ,1H),2.51-2.44(m,2H),2.40(s,1H),2.36(d,J=8.6Hz,2H),2.16-2.06(m,3H),1.9 1(dd,J=12.2,6.0Hz,1H),1.71(s,2H),1.11(t,J=7.2Hz,3H),0.66(t,J=6.8Hz,3H). 13C NMR(100MHz,CDCl3)δ166.39,164.56,163.35,153.19,151.36,137.40,132.10,13 2.10,126.93,123.27,123.26,113.61,113.61,85.23,84.14,83.30,80.44,80.29 ,78.14,77.36,61.10,59.18,58.89,58.10,56.24,56.09,55.53,54.05,50.90,49.12,49.03,48.30,45.26,42.29,39.18,37.62,36.22,35.11,26.48,15.50,13.66.

[0069] Example 29: Preparation of Compound 29 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of nicotinoyl chloride hydrochloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 52 N2O 11 Pale yellow solid (66.9 mg), yield 57.7%. HRESIMS m / z:[(M+H) + ,749.35] 1H NMR(400MHz,Chloroform-d)δ9.15(d,J=1.2Hz,1H),8.70(dd,J=4.8,1.6Hz,1H),8.21(d t,J=8.0,1.8Hz,1H),8.04(d,J=8.8Hz,2H),7.30(ddd,J=8.0,4.8,0.8Hz,1H),6.90(d,J= 8.8Hz,2H),5.29-5.26(m,1H),4.11(dd,J=8.8,5.8Hz,1H),3.98(d,J=6.8Hz,1H),3.83( s,3H),3.62(d,J=8.4Hz,1H),3.59-3.53(m,1H),3.30(s,3H),3.26(s,3H),3.24(s,3H),3 .15(s,3H),3.12(s,1H),3.03(t,J=4.6Hz,2H),3.00(s,1H),2.89(dd,J=7.4,5.2Hz,1H) ,2.58(dd,J=12.2,7.2Hz,1H),2.52(d,J=5.8Hz,1H),2.49(d,J=4.2Hz,1H),2.47(d,J=2. 8Hz,1H),2.44(t,J=6.0Hz,1H),2.29(dt,J=12.2,6.2Hz,1H),2.18-2.06(m,3H),1.98(s, 1H),1.92(dt,J=10.4,6.2Hz,1H),1.67-1.56(m,2H),1.36(s,3H),1.09(t,J=7.2Hz,3H). 13 C NMR (100MHz, CDCl3) δ169.92,166.20,164.42,163.64,153.23,151.26,137.32,13 2.02,132.02,126.73,123.23,122.53,113.91,113.91,85.52,84.81,83.48,83.34 ,80.45,80.16,76.96,61.67,59.19,58.23,57.95,56.07,55.54,53.83,50.40,49.34,49.14,49.07,43.98,41.86,39.71,39.20,35.61,35.04,26.39,21.82,13.58.

[0070] Example 30: Preparation of compound 30 100 mg of compound 3 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of nicotinoyl chloride hydrochloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was evaporated by rotation, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 38 H 49 N3O9, pale yellow solid (109.3 mg), yield 75.3%. HRESIMS m / z:[(M+H) + ,692.34] 1 H NMR(400MHz,Chloroform-d)δ9.29(d,J=1.4Hz,1H),9.16(d,J=1.4Hz,1H),8.75(dd,J=4.8,1.8Hz,1H),8.71(dd,J=4.8,1.6Hz,1H),8.35(dt,J=7.8,1.8H z,1H),8.23(dt,J=8.0,2.0Hz,1H),7.42-7.36(m,1H),7.32(dd,J=7.8,5.6H z,1H),5.39(d,J=5.2Hz,1H),4.16(t,J=7.4Hz,1H),3.99(d,J=6.6Hz,1H),3. 66(d,J=8.2Hz,1H),3.50(d,J=9.4Hz,1H),3.30(s,3H),3.29(s,6H),3.25(s ,3H),3.11(d,J=8.2Hz,1H),3.06(s,3H),2.92(s,1H),2.63-2.54(m,3H),2.4 9(d,J=9.6Hz,2H),2.44(s,1H),2.39(s,1H),2.37(d,J=3.8Hz,1H),2.16-2.0 8(m,3H),1.93(s,2H),1.84(s,1H),1.69-1.59(m,2H),1.11(t,J=7.2Hz,3H). 13C NMR(100MHz, CDCl3)δ165.38,164.48,153.31,153.28,151.59,151.32,137. 55,137.36,126.73,126.55,123.37,123.29,85.18,84.19,83.09,80.31,80. 02,78.43,77.70,61.28,59.20,58.89,58.16,56.20,53.96,50.84,49.11,48.78,48.58,48.51,45.37,42.32,39.20,36.83,36.11,35.21,26.44,13.69.

[0071] Example 31: Preparation of Compound 31 100 mg of compound 3 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-methoxybenzyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 42 H 55 NO 11 Pale yellow solid (101.5 mg), yield 64.5%. HRESIMS m / z:[(M+H) + ,750.37] 1H NMR(400MHz,Chloroform-d)δ8.07(d,J=8.8Hz,2H),7.94(d,J=8.8Hz,2H),6.91(d,J=8.8Hz,2H),6.84(d,J=8.8Hz,2H),5.30(d,J=5.2Hz,1H),4. 15(dd,J=8.8,6.2Hz,1H),4.01(d,J=6.2Hz,1H),3.84(s,3H),3.80(s,3H ),3.64(d,J=8.2Hz,1H),3.51-3.42(m,1H),3.31(s,3H),3.29(s,3H),3.2 8(s,3H),3.24(s,3H),3.13(d,J=8.2Hz,1H),3.04(s,3H),2.92(s,1H),2 .62-2.52(m,3H),2.48(dq,J=12.0,6.2,5.4Hz,2H),2.40(d,J=14.4Hz,2 H),2.32(dd,J=14.4,8.8Hz,2H),2.14-2.03(m,3H),1.89(dd,J=11.8,6.0Hz,1H),1.81(s,1H),1.64(dd,J=9.4,4.2Hz,2H),1.11(t,J=7.2Hz,3H). 13 C NMR (100MHz, CDCl3) δ166.51,165.60,163.24,163.21,132.14,132.14,131.95,131. 95,123.52,123.35,113.57,113.57,113.52,113.52,85.10,83.21,83.16,80.57,80 .40,78.45,77.42,60.96,59.19,58.75,58.22,56.21,55.48,55.48,54.21,50.86,48.97,48.63,48.44,48.38,45.27,42.44,39.16,36.85,36.28,34.97,26.42,13.65.

[0072] Example 32: Preparation of Compound 32 100 mg of compound 3 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of froyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 36 H 47 NO 11 Pale yellow solid (92.6 mg), yield 65.9%. HRESIMS m / z:[(M+H) + ,670.31] 1 H NMR(400MHz,Chloroform-d)δ7.58(dd,J=1.8,0.8Hz,1H),7.52(dd,J=1.8,0.8Hz,1 H),7.17(dd,J=3.4,0.8Hz,1H),7.11(dd,J=3.4,0.8Hz,1H),6.48(dd,J=3.4,1.6Hz ,1H),6.44(dd,J=3.4,1.6Hz,1H),5.27(d,J=5.2Hz,1H),4.11(dd,J=8.4,6.8Hz,1H ),3.98(d,J=5.8Hz,1H),3.64(d,J=8.2Hz,1H),3.50(q,J=12.2Hz,1H),3.34(s,3H), 3.29(s,3H),3.28(s,3H),3.23(s,3H),3.12(d,J=8.2Hz,1H),3.06(s,3H),3.01(dd ,J=9.8,6.2Hz,1H),2.88(s,1H),2.60-2.54(m,2H),2.53-2.47(m,2H),2.41(s,1H), 2.38(d,J=6.4Hz,1H),2.35-2.26(m,2H),2.07(d,J=6.0Hz,3H),1.91(dd,J=12.0,6 .2Hz,1H),1.63(dd,J=9.6,4.2Hz,2H),1.17(t,J=7.2Hz,1H),1.11(t,J=7.2Hz,3H). 13C NMR(100MHz,CDCl3)δ158.73,157.92,146.41,146.21,145.21,145.00,1 18.26,118.20,111.83,111.79,85.07,83.67,83.22,80.56,80.36,78.4 4,77.36,61.34,59.21,58.80,58.24,56.25,53.93,50.82,49.14,48.61 ,48.53,48.36,45.12,42.18,39.17,36.69,36.14,35.08,26.49,13.67.

[0073] Example 33: Preparation of Compound 33 100 mg of compound 1 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of froyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 39 H 51 NO 11 Pale yellow solid (73.4 mg), yield 63.7%. HRESIMS m / z:[(M+H) + ,710.34] 1H NMR(400MHz,Chloroform-d)δ8.05(d,J=8.8Hz,2H),7.51(dd,J=1.6,0.8Hz,1H),7.08(dd,J=3.4,0.8Hz,1H),6.91(d,J=8.8Hz,2H),6.42(dd,J=3. 4,1.6Hz,1H),5.25(d,J=5.2Hz,1H),4.13(dd,J=8.8,6.2Hz,1H),4.00(d, J=6.2Hz,1H),3.85(s,3H),3.64(d,J=8.4Hz,1H),3.52-3.40(m,1H),3.36 (s,3H),3.29(s,3H),3.27(s,3H),3.24(s,3H),3.13(d,J=8.2Hz,1H),3.0 2(s,3H),2.90(s,1H),2.58(dt,J=14.0,6.6Hz,2H),2.53-2.45(m,2H),2. 45-2.37(m,2H),2.32(dd,J=14.0,8.8Hz,2H),2.08(d,J=5.8Hz,3H),1.92 (s,1H),1.80-1.57(m,3H),1.26(d,J=11.6Hz,1H),1.11(t,J=7.0Hz,3H). 13 C NMR (100MHz, CDCl3) δ166.48,163.26,158.00,146.17,145.09,132.14,132.14 ,123.27,118.05,113.59,113.59,111.79,85.16,83.83,83.16,80.60,80.38, 78.37,77.36,77.28,61.42,59.21,58.79,58.28,56.28,55.51,53.96,50.83,49.16,48.64,48.42,45.18,42.31,39.18,36.81,36.13,35.09,26.48,13.69.

[0074] Example 34: Preparation of Compound 34 100 mg of compound 3 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of cyclohexanecarbonyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 40 H 63 NO9, pale yellow solid (63.9 mg), yield 43.4%. HRESIMS m / z:[(M+H) + ,702.45] 1 H NMR(400MHz,Chloroform-d)δ4.86(d,J=5.2Hz,1H),3.94(dd,J=6.6,1.6Hz,1H),3.86(t ,J=7.8Hz,1H),3.61(d,J=8.2Hz,1H),3.32(d,J=5.4Hz,1H),3.28(s,3H),3.28(s,3H),3 .26(s,3H),3.19(s,3H),3.14(s,3H),3.09(d,J=8.2Hz,1H),2.97(dd,J=9.2,6.2Hz,1H) ,2.78(s,1H),2.56-2.47(m,2H),2.46(d,J=4.4Hz,1H),2.44-2.38(m,2H),2.37(s,2H), 2.32(q,J=3.6Hz,1H),2.29(t,J=3.6Hz,1H),2.27-2.24(m,1H),2.24-2.20(m,1H),2.18 (dd,J=7.8,3.8Hz,2H),2.02(d,J=6.6Hz,1H),1.97-1.88(m,3H),1.86-1.81(m,3H),1.8 0(d,J=3.2Hz,1H),1.74-1.69(m,3H),1.61(s,2H),1.59(d,J=4.4Hz,2H),1.49-1.41(m, 2H),1.41-1.34(m,2H),1.28(d,J=3.6Hz,2H),1.24-1.18(m,3H),1.06(t,J=7.2Hz,3H). 13 C NMR(100MHz,CDCl3)δ175.97,175.28,84.81,83.31,81.89,80.35,80.18,78. 45,76.88,60.48,59.16,58.77,57.90,56.04,54.35,50.81,48.78,48.56,48 .01,47.99,44.84,43.24,43.16,42.29,39.02,36.79,36.21,34.72,29.23,29.06,29.00,28.76,26.36,26.06,26.00,25.65,25.56,25.50,25.45,13.54.

[0075] Example 35: Preparation of Compound 35 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-ethoxybenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 45 H 61 NO 11 Pale yellow solid (84.2 mg), yield 53.2%. HRESIMS m / z:[(M+H) + ,792.42] 1H NMR(400MHz,Chloroform-d)δ8.07(d,J=8.8Hz,2H),7.93(d,J=8.8Hz,2H),6.89(d,J=8.8Hz,2H),6.83(d,J=8.8Hz,2H),5.24(d,J=5.2Hz,1H),4.22-4. 12(m,1H),4.06(dq,J=14.2,7.0Hz,5H),3.63(d,J=8.2Hz,1H),3.46(d,J=9 .6Hz,1H),3.40-3.34(m,1H),3.32(s,3H),3.30(s,3H),3.27(s,3H),3.24(s ,3H),3.22-3.17(m,1H),3.09(d,J=8.2Hz,1H),3.02(dd,J=9.6,6.2Hz,1H) ,2.90(s,1H),2.65(t,J=5.2Hz,1H),2.57-2.50(m,2H),2.49-2.42(m,2H),2 .40-2.33(m,3H),2.12-2.04(m,3H),1.72(s,2H),1.67-1.59(m,2H),1.46-1 .41(m,3H),1.41-1.37(m,3H),1.10(t,J=7.0Hz,3H),0.63(t,J=7.0Hz,3H). 13 C NMR (100MHz, CDCl3) δ166.57,165.65,162.68,162.62,132.12,132.12,131.95,131.95,1 23.36,123.25,114.01,114.01,113.99,112.99,85.19,83.34,83.11,80.80,80.33,78.18 ,77.66,77.36,63.72,60.90,59.18,58.85,58.24,56.26,56.02,54.20,50.89,49.06,48.94,48.20,45.27,42.35,39.16,37.68,36.37,35.01,26.44,15.47,14.83,14.80,13.64.

[0076] Example 36: Preparation of Compound 36 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-ethoxybenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 44 H 59 NO 11 Pale yellow solid (104.3 mg), yield 84.5%. HRESIMS m / z:[(M+H) + ,778.40] 1 H NMR(400MHz,Chloroform-d)δ8.08(d,J=8.8Hz,2H),7.93(d,J=8.8Hz,2H),6.91( d,J=8.8Hz,2H),6.83(d,J=8.8Hz,2H),5.24(d,J=5.2Hz,1H),4.18-4.10(m,1H),4 .04(q,J=7.0Hz,3H),3.85(s,3H),3.63(d,J=8.2Hz,1H),3.49-3.42(m,1H),3.40- 3.34(m,1H),3.32(s,3H),3.30(s,3H),3.27(s,3H),3.24(s,3H),3.22-3.17(m,1H ),3.09(d,J=8.2Hz,1H),3.02(dd,J=9.6,6.2Hz,1H),2.90(s,1H),2.66(t,J=5.2H z,1H),2.52(d,J=6.6Hz,1H),2.48(d,J=7.2Hz,1H),2.44(t,J=6.0Hz,1H),2.41-2 .33(m,3H),2.14-2.02(m,3H),1.89(dd,J=11.6,5.8Hz,1H),1.76(s,2H),1.63(t, J=5.8Hz,2H),1.40(t,J=7.0Hz,3H),1.10(t,J=7.2Hz,3H),0.63(t,J=6.8Hz,3H). 13C NMR(100MHz,CDCl3)δ166.53,165.65,163.26,162.62,132.13,132.13,131.94,123.44 ,123.34,113.99,113.99,113.55,113.55,85.20,83.32,83.10,80.78,80.32,78.18,77 .69,77.36,63.71,60.91,59.17,58.85,58.25,56.26,56.02,55.50,54.18,50.88,49.06,48.94,48.20,45.25,42.34,39.15,37.69,36.35,35.01,26.44,15.47,14.79,13.64.

[0077] Example 37: Preparation of Compound 37 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-ethoxybenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was evaporated by rotation, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 44 H 57 NO 12 Pale yellow solid (97.9 mg), yield 79.8%. HRESIMS m / z:[(M+H) + ,792.38] 1H NMR(400MHz,Chloroform-d)δ8.07(d,J=8.8Hz,2H),7.93(d,J=8.8Hz,2H),6.92(d,J=8.8Hz,2H),6.83(d,J=8.8Hz,2H),5.27(d,J=5.2Hz,1H),4.15(dd,J=8 .8,5.6Hz,1H),4.04(q,J=7.0Hz,2H),3.99(d,J=6.6Hz,1H),3.85(s,3H),3.63 (d,J=8.4Hz,1H),3.52(d,J=10.8Hz,1H),3.33(s,3H),3.28(s,3H),3.25(s,3H ),3.16(s,3H),3.06(d,J=8.8Hz,1H),3.03(s,3H),3.01(d,J=5.8Hz,1H),2.8 9(s,1H),2.62-2.57(m,1H),2.54(t,J=6.6Hz,1H),2.51(d,J=5.2Hz,1H),2.48 (d,J=6.4Hz,1H),2.44(t,J=3.4Hz,1H),2.11(d,J=6.4Hz,2H),1.92(d,J=5.8H z,1H),1.64(s,4H),1.40(t,J=7.0Hz,3H),1.35(s,3H),1.11(t,J=7.2Hz,3H). 13 C NMR (100MHz, CDCl3) δ170.01,166.42,165.56,163.61,162.72,132.13,132.13,131.96, 131.96,123.18,122.78,114.02,114.02,113.91,113.91,85.73,84.85,83.42,82.54,8 0.56,77.36,77.33,63.75,61.56,59.26,58.44,57.97,56.17,55.59,54.01,50.45,49.34,49.12,44.08,41.99,39.86,39.25,35.83,35.05,29.84,26.41,21.89,14.80,13.62.

[0078] Example 38: Preparation of Compound 38 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-nitrobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 51 N3O 13 Pale yellow solid (109.0 mg), yield 68.7%. HRESIMS m / z:[(M+H) + ,794.34] 1 H NMR(400MHz,Chloroform-d)δ8.30(td,J=9.8,1.0Hz,4H),8.23(d,J=8.8Hz,2H),8.15(d,J=9.0Hz,2H),5.33(d,J=5.2Hz,1H),4.17(dd, J=8.8,5.8Hz,1H),4.02(d,J=6.6Hz,1H),3.67(d,J=8.2Hz,1H),3.56-3.47(m,1H),3.45-3.39(m,1H),3.30(s,3H),3.30(s,3H),3.28(s, 3H),3.25(s,3H),3.22-3.17(m,1H),3.05(dd,J=10.4,7.0Hz,2H),2.91(s,1H),2.71(t,J=5.4Hz,1H),2.56-2.47(m,3H),2.45-2.40(m, 2H),2.40-2.30(m,2H),2.20-2.08(m,3H),1.95(dd,J=11.2,6.2Hz,1H),1.70-1.59(m,3H),1.11(t,J=7.2Hz,3H),0.64(t,J=6.8Hz,3H). 13C NMR(100MHz,CDCl3)δ164.65,163.90,150.62,150.56,136.32,136.32,136.15,13 6.15,131.17,131.02,123.63,123.63,123.56,123.56,85.29,84.56,83.15,80.20 ,80.13,78.35,78.20,77.36,61.36,59.18,59.01,58.19,56.21,53.83,50.89,49.29,49.14,48.40,45.33,42.21,39.22,37.68,36.07,35.34,26.47,15.65,13.69.

[0079] Example 39: Preparation of Compound 39 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-nitrobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 42 H 54 N2O 12 Pale yellow solid (73.9 mg), yield 59.8%. HRESIMS m / z:[(M+H) + ,779.36] 1H NMR(400MHz,Chloroform-d)δ8.19(dd,J=9.0,9.0Hz,4H),8.07(d,J=8.8Hz,2H),6. 91(d,J=8.8Hz,2H),5.29(d,J=5.2Hz,1H),4.17-4.08(m,1H),4.04(d,J=7.8Hz,1H) ,3.85(s,3H),3.65(d,J=8.2Hz,1H),3.53(q,J=12.0Hz,1H),3.44-3.37(m,1H),3.3 0(s,3H),3.29(s,3H),3.28(s,3H),3.25(s,3H),3.22(d,J=8.4Hz,1H),3.09(d,J=8. 2Hz,1H),3.04(dd,J=9.8,6.2Hz,1H),2.89(s,1H),2.67(t,J=5.2Hz,1H),2.55(t,J =6.0Hz,1H),2.52(s,1H),2.49(d,J=3.2Hz,1H),2.46(d,J=4.8Hz,1H),2.41(s,1H), 2.40-2.35(m,2H),2.35-2.29(m,1H),2.16-2.06(m,3H),1.92(dd,J=11.0,5.6Hz,1 H),1.72(s,1H),1.64(d,J=5.8Hz,1H),1.11(t,J=7.2Hz,3H),0.68(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ166.37,163.98,163.40,150.46,136.53,132.07,132.07,131. 06,131.06,123.49,123.49,123.20,113.63,113.63,85.26,84.52,83.26,80.27,78 .12,77.36,77.26,61.20,59.17,58.89,58.04,56.22,56.12,55.52,53.98,50.89,49.14,49.06,48.32,45.32,42.24,39.17,37.60,36.14,35.15,26.49,15.51,13.66.

[0080] Example 40: Preparation of compound 40 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-nitrobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 42 H 52 N2O 13 Pale yellow solid (85.1 mg), yield 69.3%. HRESIMS m / z:[(M+H) + ,793.34] 1 H NMR(400MHz,Chloroform-d)δ8.18(dd,J=28.0,8.8Hz,4H),8.05(d,J=8.8Hz,2H),6.92(d,J=8.8Hz,2H),5.31(d,J=5.2Hz,1H),4.12(dd,J=8.8,5.8Hz,1 H),4.00(d,J=6.6Hz,1H),3.85(s,3H),3.64(d,J=8.4Hz,1H),3.62-3.56(m, 1H),3.30(s,3H),3.28(s,3H),3.26(s,3H),3.17(s,3H),3.15(d,J=8.4Hz,1 H),3.10-3.06(m,1H),3.05(s,1H),3.01(s,1H),2.93-2.88(m,1H),2.59(dd ,J=12.0,7.2Hz,1H),2.54(d,J=5.8Hz,1H),2.51(s,1H),2.49(s,1H),2.46( t,J=6.0Hz,1H),2.37-2.27(m,1H),2.14(dd,J=10.4,6.2Hz,3H),2.00-1.90 (m,1H),1.69(s,1H),1.66-1.60(m,2H),1.39(s,3H),1.11(t,J=7.2Hz,3H). 13C NMR(100MHz,CDCl3)δ169.96,166.24,163.90,163.74,150.52,136.35,132.05,132. 05,131.05,131.05,123.52,123.52,122.51,113.98,113.98,85.50,84.88,83.90,8 3.37, 80.47, 80.06, 76.93, 61.81, 59.24, 58.23, 58.01, 56.11, 55.60, 53.82, 50.45, 49.39, 49.22, 49.13, 44.07, 41.86, 39.73, 39.24, 35.58, 35.12, 26.44, 21.86, 13.63.

[0081] Example 41: Preparation of Compound 41 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, twice the equivalent volume of acetyl chloride was added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 31 H 49 NO9, pale yellow solid (89.6 mg), yield 77.3%. HRESIMS m / z:[(M+H) + ,580.34] 1H NMR(400MHz,Chloroform-d)δ4.79(d,J=5.2Hz,1H),3.97(d,J=5.2Hz,1H),3. 93-3.87(m,1H),3.62(d,J=8.2Hz,1H),3.50-3.45(m,1H),3.37(d,J=6.0Hz,1 H),3.34(dd,J=6.8,1.6Hz,1H),3.31(s,3H),3.28(s,6H),3.21(s,3H),3.06( d,J=8.2Hz,1H),2.98(dd,J=9.6,6.2Hz,1H),2.76(s,1H),2.53(d,J=5.4Hz,1H ),2.50(d,J=4.6Hz,1H),2.48-2.45(m,2H),2.44(s,1H),2.37(s,1H),2.27-2 .21(m,1H),2.18(dd,J=13.8,7.2Hz,1H),2.07(s,3H),2.04(s,3H),1.95(ddd, J=12.2,7.2,5.0Hz,1H),1.89(d,J=6.0Hz,1H),1.86(d,J=2.6Hz,1H),1.83(s ,2H),1.61(q,J=6.2,3.8Hz,2H),1.11(t,J=7.0Hz,3H),1.07(t,J=7.2Hz,3H). 13 C NMR (100MHz, CDCl3) δ171.46,170.43,85.07,83.34,82.27,80.40,80.22,78.29,77.69,61.10,59.14,58.88,58.10,56.18 ,56.14,53.93,50.80,49.03,48.89,48.05,44.56,41.88,39.08,37.47,36.36,34.95,26.43,21.59,21.50,16.29,13.56.

[0082] Example 42: Preparation of Compound 42 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent amounts of acetyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 37 H 53 NO 10 Pale yellow solid (54.6 mg), yield 51.2%. HRESIMS m / z:[(M+H) + ,672.36] 1 H NMR(400MHz,Chloroform-d)δ8.04(d,J=8.8Hz,2H),6.90(d,J=8.8Hz,2H),5.03(d,J=5.2Hz,1H),4.03-3.96(m,2H),3.85(s,3H) ,3.61(d,J=8.2Hz,1H),3.37(s,3H),3.32(s,1H),3.28(s,3H),3.24(d,J=5.0Hz,6H),3.17-3.11(m,1H),3.08(d,J=8.4Hz,1H),3 .00(dd,J=9.8,6.4Hz,1H),2.82(s,1H),2.61(t,J=6.2Hz,1H),2.56-2.40(m,4H),2.33(d,J=12.0Hz,2H),2.31-2.24(m,2H),2.0 5(d,J=6.4Hz,1H),2.02(s,3H),2.01-1.83(m,3H),1.77(s,1H),1.67-1.58(m,2H),1.08(t,J=7.2Hz,3H),0.55(t,J=6.8Hz,3H). 13C NMR(100MHz,CDCl3)δ170.59,166.38,163.23,132.09,132.09,123.44,11 3.51,113.51,85.28,83.24,82.82,80.48,80.30,78.07,77.53,61.33,59 .16,58.83,58.12,56.24,55.94,55.50,53.92,50.84,49.09,49.09,48.3 2,45.04,42.17,39.16,37.48,36.27,35.11,26.48,21.61,15.35,13.65.

[0083] Example 43: Preparation of Compound 43 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of acetyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 37 H 51 NO 11 Pale yellow solid (91.7 mg), yield 86.3%. HRESIMS m / z:[(M+H) + ,686.34] 1H NMR(400MHz,Chloroform-d)δ8.03(d,J=8.9Hz,2H),6.91(d,J=8.9Hz,2H),5.07(d,J=5.2Hz,1H),3.99(dd,J=8.9,5.8Hz,1H),3.94(d, J=6.7Hz,1H),3.85(s,3H),3.61(d,J=8.5Hz,1H),3.37(s,3H),3.26(s,3H),3.23(s,3H),3.13(s,3H),3.02-2.97(m,3H),2.95(d,J=3. 8Hz,1H),2.86-2.80(m,1H),2.59-2.53(m,1H),2.46(t,J=2.7Hz,3H),2.42(d,J=5.9Hz,1H),2.28(ddt,J=12.3,5.9,2.8Hz,1H),2.07( dd,J=6.4,4.8Hz,2H),2.03(s,3H),2.00-1.91(m,2H),1.82(s,2H),1.63-1.57(m,2H),1.36(s,1H),1.24(s,1H),1.08(t,J=7.1Hz,3H). 13 C NMR(100MHz,CDCl3)δ170.52,169.99,166.24,163.57,132.06,132.06,12 2.64,113.86,113.86,85.59,84.89,83.29,82.22,80.46,80.14,77.09,6 1.92,59.21,58.28,57.94,56.15,55.56,53.72,50.36,49.26,49.04,43. 83,41.76,39.66,39.19,35.68,35.05,26.38,22.78,21.77,21.55,13.60.

[0084] Example 44: Preparation of Compound 44 100 mg of compound 3 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, twice the equivalent volume of acetyl chloride was added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows.

change

[0085] Example 45: Preparation of Compound 45 100 mg of compound 1 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent amounts of acetyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 36 H 51 NO 10 Pale yellow solid (84.7 mg), yield 79.3%. HRESIMS m / z:[(M+H) + ,658.35] 1 H NMR(400MHz,Chloroform-d)δ8.02(d,J=8.8Hz,2H),6.91(d,J=8.8Hz,2H),5.29(s,1H),5.08(d,J=5.2Hz,1H),4.04-3.98(m,1H),3.96(d, J=6.0Hz,1H),3.84(s,3H),3.61(d,J=8.2Hz,1H),3.37(s,3H),3.33(d,J=4.8Hz,1H),3.28(s,3H),3.25(s,3H),3.23(s,3H),3.12(d,J=8. 2Hz,1H),3.00(dd,J=9.8,6.2Hz,1H),2.96(s,3H),2.84(s,1H),2.58-2.51(m,2H),2.49-2.42(m,2H),2.36(s,1H),2.35-2.18(m,3H),2.0 4(d,J=6.6Hz,1H),2.01(s,3H),1.96(d,J=14.6Hz,1H),1.93-1.85(m,1H),1.79(s,1H),1.62(dd,J=8.8,3.8Hz,2H),1.09(t,J=7.2Hz,3H). 13C NMR(100MHz,CDCl3)δ170.57,166.46,163.21,132.10,132.10,123.32,113.54,113.54,85.19,83.11,82.79,80.36,80.32,78.33,77.33,61.39 ,59.18,58.74,58.13,56.20,55.49,53.94,50.80,49.12,48.54,48.54 ,48.40,45.01,42.23,39.15,36.68,36.19,35.04,26.45,21.59,13.67.

[0086] Example 46: Preparation of Compound 46 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of 4-trifluoromethylbenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 43 H 51 F6NO9, pale yellow solid (106.4 mg), yield 63.4%. HRESIMS m / z:[(M+H) + ,840.34] 1H NMR(400MHz,Chloroform-d)δ8.25(d,J=8.0Hz,2H),8.10(d,J=8.0Hz,2H),7.7 0(d,J=8.2Hz,2H),7.64(d,J=8.2Hz,2H),5.31(d,J=5.2Hz,1H),4.16(d,J=14.8 Hz,1H),4.03(d,J=5.0Hz,1H),3.66(d,J=8.2Hz,1H),3.51(q,J=10.4,8.6Hz,1 H),3.43-3.37(m,1H),3.30(s,3H),3.30(s,3H),3.28(s,3H),3.25(s,3H),3.21 -3.16(m,1H),3.09-3.06(m,1H),3.06-3.02(m,1H),2.91(s,1H),2.70(t,J=5. 0Hz,1H),2.59-2.52(m,2H),2.52-2.46(m,2H),2.42(s,1H),2.39-2.34(m,2H), 2.34-2.29(m,1H),2.13(d,J=9.2Hz,3H),1.92(dd,J=11.6,5.8Hz,1H),1.65(t ,J=4.4Hz,1H),1.44-1.32(m,1H),1.11(t,J=7.2Hz,3H),0.62(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ165.37,164.61,134.54,134.43,134.22,134.18,134.11,134.01 ,130.46,130.29,125.49,125.45,125.41,125.37,125.20,125.18,122.49,122.47,85. 23,84.11,83.20,80.26,80.22,78.19,78.13,61.21,59.16,58.95,58.15,56.21,56.14,53.96,50.89,49.21,49.08,45.26,42.26,39.19,37.66,36.11,26.44,15.48,13.64.

[0087] Example 47: Preparation of Compound 47 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of 4-trifluoromethylbenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 43 H 54 F3NO 10 Pale yellow solid (61.7 mg), yield 48.5%. HRESIMS m / z:[(M+H) + ,802.37] 1 H NMR(400MHz,Chloroform-d)δ8.10(d,J=8.2Hz,2H),8.07(d,J=8.8Hz,2H),7.62( d,J=8.2Hz,2H),6.91(d,J=9.0Hz,2H),5.27(d,J=5.2Hz,1H),4.17-4.09(m,1H),4 .04(d,J=5.2Hz,1H),3.84(s,3H),3.64(d,J=8.2Hz,1H),3.56-3.45(m,1H),3.42 -3.37(m,1H),3.30(s,6H),3.28(s,3H),3.25(s,3H),3.24-3.18(m,1H),3.09(d,J =8.2Hz,1H),3.04(dd,J=9.6,6.2Hz,1H),2.89(s,1H),2.67(t,J=5.2Hz,1H),2.5 5(dd,J=7.0,5.0Hz,1H),2.51(d,J=12.8Hz,2H),2.47(d,J=3.0Hz,1H),2.41(s,1H) ),2.37(t,J=7.0Hz,2H),2.35-2.28(m,1H),2.11(d,J=6.4Hz,3H),1.91(dd,J=12. 2,6.0Hz,2H),1.64(d,J=3.4Hz,1H),1.11(t,J=7.2Hz,3H),0.66(t,J=6.8Hz,3H). 13C NMR(100MHz,CDCl3)δ166.41,164.67,163.35,134.29,133.98,132.08,132.08,130.3 3,130.33,125.35,125.31,123.26,122.50,113.59,113.59,85.20,84.07,83.26,80.3 9, 80.25, 78.14, 77.38, 61.10, 59.16, 58.87, 58.08, 56.22, 56.09, 55.50, 54.06, 50.88, 49.11, 49.02, 48.21, 45.25, 42.26, 39.15, 37.62, 36.16, 35.04, 26.44, 15.48, 13.62.

[0088] Example 48: Preparation of Compound 48 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of 4-trifluoromethylbenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 43 H 52 F3NO 11 Pale yellow solid (96.7 mg), yield 76.5%. HRESIMS m / z:[(M+H) + ,816.34] 1H NMR(400MHz,Chloroform-d)δ8.08(d,J=8.0Hz,2H),8.04(d,J=9.0Hz,2H),7.62(d ,J=8.0Hz,2H),6.90(d,J=9.0Hz,2H),5.29(d,J=5.2Hz,1H),4.13(dd,J=8.8,5.8Hz ,1H),3.99(d,J=6.6Hz,1H),3.83(s,3H),3.63(d,J=8.4Hz,1H),3.57(dd,J=13.8, 3.8Hz,1H),3.30(s,3H),3.27(s,3H),3.25(s,3H),3.16(s,3H),3.14(d,J=8.4Hz,1 H),3.10-3.04(m,1H),3.04-2.99(m,3H),2.90(t,J=5.8Hz,1H),2.59(dd,J=12.0, 7.2Hz,1H),2.53(s,1H),2.50(d,J=4.2Hz,1H),2.48(s,1H),2.45(t,J=6.0Hz,1H), 2.37-2.25(m,1H),2.14(d,J=6.0Hz,2H),2.11(d,J=4.0Hz,1H),1.93(dd,J=10.6, 6.2Hz,1H),1.89(s,1H),1.63(d,J=4.2Hz,1H),1.37(s,3H),1.10(t,J=7.2Hz,3H). 13 C NMR (100MHz, CDCl3) δ169.96,166.26,164.56,163.66,134.38,134.08,134.06,132.03 ,132.03,130.29,130.29,125.35,125.31,122.53,113.91,113.91,85.54,84.85,83.4 5,83.35,80.45,80.15,77.02,61.70,59.20,58.24,57.96,56.09,55.54,53.85,50.41,49.32,49.17,49.08,44.01,41.86,39.74,39.21,35.59,35.05,26.39,21.82,13.57.

[0089] Example 49: Preparation of Compound 49 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of isonicotinoyl chloride hydrochloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 39 H 51 N3O9, pale yellow solid (94.4 mg), yield 66.9%. HRESIMS m / z:[(M+H) + ,706.36] 1 H NMR(400MHz,Chloroform-d)δ8.77(dd,J=4.4,1.6Hz,2H),8.71(dd,J=4.4,1.6H z,2H),7.93(dd,J=4.4,1.6Hz,2H),7.78(dd,J=4.4,1.6Hz,2H),5.28(d,J=5.4Hz ,1H),4.14(dd,J=8.8,6.2Hz,1H),4.00(d,J=8.2Hz,1H),3.65(d,J=8.4Hz,1H), 3.50(q,J=12.2Hz,1H),3.39(dd,J=8.4,6.8Hz,1H),3.29(s,3H),3.29(s,3H),3. 27(s,3H),3.23(s,3H),3.18(dd,J=8.4,7.0Hz,1H),3.03(dd,J=14.4,7.4Hz,2H ),2.88(s,1H),2.68(t,J=5.6Hz,1H),2.53(dd,J=11.8,7.2Hz,2H),2.48(d,J=5. 6Hz,1H),2.43(d,J=19.8Hz,2H),2.39-2.28(m,3H),2.11(t,J=5.6Hz,3H),1.92( d,J=6.4Hz,1H),1.68-1.57(m,2H),1.10(t,J=7.2Hz,3H),0.62(t,J=6.8Hz,3H). 13C NMR(100MHz,CDCl3)δ165.06,164.30,150.65,150.65,150.59,150.59,138.06 ,137.88,123.29,123.29,123.18,123.18,85.23,84.36,83.15,80.19,80.11, 78.26, 78.16, 61.24, 59.14, 58.95, 58.14, 56.18, 56.16, 53.85, 50.85, 49.21, 49.08, 48.35, 45.19, 42.17, 39.18, 37.62, 36.00, 35.27, 26.45, 15.52, 13.65.

[0090] Example 50: Preparation of Compound 50 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of isonicotinoyl chloride hydrochloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 54 N2O 10 Pale yellow solid (79.1 mg), yield 67.8%. HRESIMS m / z:[(M+H) + ,735.37] 1H NMR(400MHz,Chloroform-d)δ8.70(dd,J=4.4,1.8Hz,2H),8.07(d,J=8.8Hz,2H),7 .80(dd,J=4.6,1.6Hz,2H),6.91(d,J=8.8Hz,2H),5.26(d,J=5.2Hz,1H),4.14-4.08 (m,1H),4.04(d,J=5.8Hz,1H),3.85(s,3H),3.64(d,J=8.2Hz,1H),3.56-3.47(m,1H ),3.44-3.36(m,1H),3.30(s,3H),3.29(s,3H),3.28(s,3H),3.24(s,3H),3.23-3.1 7(m,1H),3.09(d,J=8.2Hz,1H),3.03(dd,J=9.8,6.2Hz,1H),2.88(s,1H),2.67(t,J =5.6Hz,1H),2.52(t,J=3.4Hz,1H),2.48(d,J=3.2Hz,1H),2.46(s,1H),2.44-2.36( m,3H),2.36-2.31(m,1H),2.10(d,J=6.1Hz,3H),1.92(dd,J=11.6,6.0Hz,1H),1.78 (s,1H),1.65(dd,J=12.4,5.2Hz,2H),1.11(t,J=7.2Hz,3H),0.67(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ166.36,164.40,163.37,150.55,150.55,138.25,132.08,13 2.08,123.28,123.28,123.25,113.62,113.62,85.24,84.40,83.26,80.28,80.28 ,78.12,77.27,61.15,59.17,58.88,58.05,56.22,56.10,55.52,54.00,50.88,49.13,49.04,48.31,45.29,42.24,39.17,37.60,36.10,35.13,26.48,15.50,13.66.

[0091] Example 51: Preparation of Compound 51 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of isonicotinoyl chloride hydrochloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 52 N2O 11 Pale yellow solid (88.7 mg), yield 76.5%. HRESIMS m / z:[(M+H) + ,749.35] 1 H NMR(400MHz,Chloroform-d)δ8.70(dd,J=4.4,1.6Hz,2H),8.04(d,J=8.8Hz,2H),7.78(dd,J=4.4,1.6Hz,2H),6.91(d,J=8.8Hz,2H),5.28(d,J=5.2Hz,1H),4 .11(dd,J=8.8,5.8Hz,1H),3.99(d,J=6.8Hz,1H),3.84(s,3H),3.63(d,J=8.4 Hz,1H),3.57(dd,J=14.2,4.4Hz,1H),3.29(s,3H),3.27(s,3H),3.25(s,3H),3 .16(s,3H),3.14(d,J=8.4Hz,1H),3.03(t,J=4.8Hz,2H),3.00(s,1H),2.92-2 .87(m,1H),2.58(dd,J=12.2,7.2Hz,1H),2.52(d,J=5.8Hz,1H),2.51-2.46(m, 2H),2.46-2.42(m,1H),2.31(dt,J=15.4,5.6Hz,1H),2.19-2.05(m,3H),1.93( dd,J=19.4,7.4Hz,2H),1.67-1.58(m,2H),1.37(s,3H),1.10(t,J=7.2Hz,3H). 13C NMR(100MHz,CDCl3)δ169.93,166.21,164.29,163.69,150.55,150.55,138.06,13 2.04,132.04,123.21,123.21,122.52,113.94,113.94,85.49,84.84,83.77,83.35 ,80.46,80.04,76.91,61.74,59.21,58.22,57.97,56.08,55.57,53.82,50.41,49.37,49.18,49.10,44.02,41.84,39.71,39.22,35.51,35.09,26.41,21.83,13.60.

[0092] Example 52: Preparation of Compound 52 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, 2 equivalents of benzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was evaporated by rotation, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 53 NO9, pale yellow solid (77.7 mg), yield 55.2%.

[0093] HRESIMS m / z:[(M+H) + ,704.37] 1H NMR(400MHz,Chloroform-d)δ8.14(dd,J=8.4,1.4Hz,2H),8.00(dd,J=8.4,1.4Hz,2H),7.56 -7.51(m,1H),7.51-7.46(m,1H),7.42(t,J=7.6Hz,2H),7.38(d,J=8.0Hz,2H),5.29(d,J=5.2 Hz,1H),4.21-4.14(m,1H),4.04(d,J=6.4Hz,1H),3.64(d,J=8.2Hz,1H),3.56-3.45(m,1H), 3.40-3.35(m,1H),3.33(s,3H),3.30(s,3H),3.28(s,3H),3.25(s,3H),3.22-3.16(m,1H),3. 09(d,J=8.2Hz,1H),3.04(dd,J=9.6,6.2Hz,1H),2.91(s,1H),2.70(t,J=5.6Hz,1H),2.53(s ,1H),2.49(d,J=6.4Hz,1H),2.45(dd,J=7.2,2.8Hz,1H),2.40(s,2H),2.37(d,J=10.6Hz,1H) ,2.33(dd,J=8.8,5.0Hz,1H),2.10(d,J=6.2Hz,3H),1.90(dt,J=11.0,5.4Hz,1H),1.82(s,1H ),1.64(q,J=3.4Hz,1H),1.33(d,J=2.8Hz,1H),1.11(t,J=7.2Hz,3H),0.59(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ166.72,165.86,132.78,132.69,131.03,130.82,130.11,13 0.11,129.93,129.93,128.30,128.30,128.30,128.30,85.20,83.43,83.29,80.61 ,80.29,78.19,77.86,60.97,59.16,58.86,58.19,56.23,56.03,54.11,50.88,49.08,48.96,48.24,45.20,42.31,39.15,37.64,36.27,35.06,26.44,15.33,13.64.

[0094] Example 53: Preparation of Compound 53 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, 2 equivalents of benzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 42 H 55 NO 10 Pale yellow solid (92.7 mg), yield 79.6%. 1 H NMR(400MHz,Chloroform-d)δ8.08(d,J=8.9Hz,2H),8.00(dd,J=8.3,1.4Hz,2H),7.52 -7.46(m,1H),7.37(dd,J=8.4,7.1Hz,2H),6.91(d,J=8.9Hz,2H),5.25(d,J=5.2Hz,1H) ,4.16(dd,J=8.5,6.6Hz,1H),4.04(d,J=6.3Hz,1H),3.85(s,3H),3.64(d,J=8.2Hz,1H ),3.49(q,J=12.2Hz,1H),3.38(dd,J=8.2,6.8Hz,1H),3.33(s,3H),3.30(s,3H),3.27( s,3H),3.24(s,3H),3.23-3.17(m,1H),3.09(d,J=8.2Hz,1H),3.03(dd,J=9.7,6.2Hz, 1H),2.90(s,1H),2.67(dt,J=5.8,3.1Hz,1H),2.57-2.51(m,2H),2.47(q,J=5.4,4.1Hz ,2H),2.41-2.34(m,3H),2.09(d,J=7.2Hz,2H),1.90(dd,J=11.9,5.5Hz,1H),1.77(s,2 H),1.66-1.62(m,1H),1.43-1.32(m,1H),1.11(t,J=7.1Hz,3H),0.63(t,J=6.9Hz,3H). 13C NMR(100MHz,CDCl3)δ166.50,165.87,163.26,132.69,132.11,132.11,131.02,129. 94,129.94,128.29,128.29,123.36,113.55,113.55,85.20,83.40,83.28,80.64,80 .28,78.16,77.59,60.96,59.17,58.86,58.22,56.28,56.03,55.51,54.13,50.86,49.03,48.96,48.15,45.21,42.28,39.13,37.69,36.26,35.02,26.43,15.47,13.64.

[0095] Example 54: Preparation of Compound 54 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of benzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 42 H 53 NO 11 Pale yellow solid (52.0 mg), yield 44.9%. HRESIMS m / z:[(M+H) + ,748.36] 1H NMR(400MHz,Chloroform-d)δ8.06(d,J=8.8Hz,2H),7.98(dd,J=8.4,1.2Hz,2H) ,7.53-7.46(m,1H),7.36(dd,J=8.4,7.2Hz,2H),6.91(d,J=9.0Hz,2H),5.28(d, J=5.2Hz,1H),4.16(dd,J=9.0,5.8Hz,1H),3.99(d,J=6.6Hz,1H),3.84(s,3H),3 .63(d,J=8.4Hz,1H),3.58-3.51(m,1H),3.32(s,3H),3.27(s,3H),3.25(s,3H), 3.16(s,3H),3.14(s,1H),3.03(dd,J=4.2,2.6Hz,3H),2.90(dt,J=7.6,3.3Hz,1 H),2.58(dd,J=12.2,7.2Hz,1H),2.55-2.51(m,1H),2.51-2.46(m,2H),2.46-2. 41(m,1H),2.33-2.24(m,1H),2.18-2.06(m,3H),1.97-1.88(m,1H),1.86(s,1H) ,1.61(dt,J=13.0,4.2Hz,2H),1.35(s,3H),1.27(s,1H),1.10(t,J=7.2Hz,3H). 13 C NMR (100MHz, CDCl3) δ169.98,166.34,165.75,163.58,132.78,132.07,132.07,130. 82,129.89,129.89,128.30,128.30,122.63,113.87,113.87,85.63,84.82,83.34,8 2.80,80.47,80.37,77.19,61.58,59.21,58.37,57.95,56.14,55.55,53.91,50.39,49.25,49.11,49.02,43.99,41.88,39.79,39.18,35.69,35.01,26.37,21.83,13.59.

[0096] Example 55: Preparation of Compound 55 100 mg of compound 3 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, 2 equivalents of benzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 40 H 51 NO9, pale yellow solid (91.5 mg), yield 63.2%. HRESIMS m / z:[(M+H) + ,690.35] 1 H NMR(400MHz,Chloroform-d)δ8.13(dd,J=8.2,1.4Hz,2H),8.00(dd,J=8.4,1.4Hz,2H),7.56-7.51(m,1H),7.51-7.46(m,1H),7.43(t,J=7.6Hz, 2H),7.36(t,J=7.6Hz,2H),5.35(d,J=5.2Hz,1H),4.18(dd,J=9.2,5.8Hz,1H),4.01(dd,1H),3.65(d,J=8.2Hz,1H),3.56-3.46(m,1H),3.33(s,3 H),3.30(s,3H),3.29(s,3H),3.25(s,3H),3.14(d,J=8.2Hz,1H),3.03( s,4H),2.94(s,1H),2.64-2.59(m,1H),2.59-2.51(m,2H),2.52-2.46(m ,2H),2.46-2.40(m,2H),2.34(m,2H),2.13-2.06(m,3H),1.91(m,1H),1 .70(t,J=3.6Hz,1H),1.65(dd,J=9.2,4.4Hz,2H),1.12(t,J=7.2Hz,3H). 13C NMR(100MHz,CDCl3)δ166.79,165.87,132.74,132.70,131.01,130.81,130.14,1 30.14,129.95,129.95,128.33,128.33,128.30,128.30,85.15,83.48,83.21,80 .45,80.40,78.47,77.65,61.05,59.21,58.80,58.21,56.23,54.16,50.87,49.02,48.64,48.51,48.43,45.26,42.41,39.19,36.84,36.25,35.04,26.45,13.68.

[0097] Example 56: Preparation of Compound 56 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-methylbenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 43 H 57 NO9, pale yellow solid (104.3 mg), yield 71.3%. HRESIMS m / z:[(M+H) + ,732.40] 1H NMR(400MHz,Chloroform-d)δ7.99(d,J=2.4Hz,2H),7.87(d,J=8.2Hz,2H),7.22 (d,J=8.0Hz,2H),7.17(d,J=7.8Hz,2H),5.90(s,2H),5.26(d,J=5.2Hz,1H),4.1 3-4.05(m,2H),3.59(d,J=8.2Hz,1H),3.39-3.33(m,1H),3.31(s,3H),3.30(s,3 H),3.27(s,3H),3.27(s,3H),3.23-3.18(m,1H),3.18-3.13(m,1H),3.04(s,1H), 3.02(d,J=8.0Hz,1H),2.93(d,J=11.2Hz,1H),2.77(d,J=11.2Hz,1H),2.75-2.7 0(m,1H),2.68(t,J=6.2Hz,1H),2.42(d,J=1.8Hz,1H),2.39(s,3H),2.37(s,3H), 2.35(s,3H),2.24(d,J=6.4Hz,1H),2.18(d,J=4.6Hz,2H),1.91-1.82(m,1H),1. 76-1.63(m,1H),1.42-1.32(m,1H),1.23(t,J=5.8Hz,3H),0.64(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ166.62,166.05,143.52,143.45,142.45,130.09,130.06,129.9 4,129.09,129.04,128.82,127.96,127.83,83.38,82.85,82.62,80.59,79.33,78.21 ,78.21,60.76,59.13,58.87,58.31,56.30,56.11,55.11,50.96,49.08,49.04,45.40,44.48,41.87,38.74,37.74,36.09,31.98,24.85,21.79,21.72,21.68,15.33,12.41.

[0098] Example 57: Preparation of Compound 57 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-methylbenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 43 H 57 NO 10 Pale yellow solid (85.9 mg), yield 72.4%. HRESIMS m / z:[(M+H) + ,748.39] 1 H NMR(400MHz,Chloroform-d)δ8.08(d,J=8.8Hz,2H),7.88(d,J=8.2Hz,2H),7.16(d ,J=8.2Hz,2H),6.91(d,J=8.8Hz,2H),5.24(d,J=5.2Hz,1H),4.15(dd,J=8.4,6.4H z,1H),4.04(dd,J=6.4,1.6Hz,1H),3.84(s,3H),3.64(d,J=8.2Hz,1H),3.49-3.45 (m,1H),3.37(dd,J=8.2,6.8Hz,1H),3.32(s,3H),3.30(s,3H),3.27(s,3H),3.24(s ,3H),3.22-3.17(m,1H),3.09(d,J=8.2Hz,1H),3.03(dd,J=9.6,6.2Hz,1H),2.90( s,1H),2.67(td,J=5.8,1.4Hz,1H),2.57-2.50(m,2H),2.49-2.42(m,2H),2.41-2. 37(m,2H),2.36(d,J=3.5Hz,3H),2.11-2.07(m,2H),1.89(q,J=6.2Hz,1H),1.68-1 .60(m,2H),1.37(s,1H),1.28(s,2H),1.10(t,J=7.2Hz,3H),0.62(t,J=6.8Hz,3H). 13C NMR(100MHz,CDCl3)δ166.50,165.91,163.22,143.22,132.09,132.09,129.95,129.9 5,128.97,128.97,128.30,123.38,113.52,113.52,85.16,83.27,83.21,80.67,80.28 ,78.14,77.63,60.90,59.15,58.83,58.20,56.25,55.99,55.48,54.14,50.84,48.92,48.12,45.19,42.30,39.11,37.67,36.26,35.00,29.81,26.41,21.73,15.45,13.63.

[0099] Example 58: Preparation of Compound 58 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-methylbenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 43 H 55 NO 11 Pale yellow solid (86.7 mg), yield 73.5%. HRESIMS m / z:[(M+H) + ,762.37] 1H NMR(400MHz,Chloroform-d)δ8.07(d,J=8.8Hz,2H),7.87(d,J=8.2Hz,2H),7.16(d,J=8.0Hz,2H),6.91(d,J=8.8Hz,2H),5.27(d,J=5.2Hz,1H),4.14 (dt,J=10.2,5.0Hz,1H),3.99(d,J=6.6Hz,1H),3.84(s,3H),3.63(d,J=8. 4Hz,1H),3.55-3.50(m,1H),3.32(s,3H),3.28(s,3H),3.24(s,3H),3.16(s ,3H),3.02(d,J=6.4Hz,3H),2.91-2.86(m,1H),2.62-2.55(m,1H),2.51(d d,J=10.4,5.2Hz,2H),2.46(dd,J=11.2,4.4Hz,2H),2.36(s,3H),2.33-2.2 4(m,1H),2.17-2.05(m,3H),1.92(d,J=3.8Hz,1H),1.62(dt,J=11.0,3.8H z,2H),1.42-1.36(m,1H),1.34(s,3H),1.28(s,1H),1.10(t,J=7.2Hz,3H). 13 C NMR (100MHz, CDCl3) δ169.98,166.38,165.82,163.57,143.37,132.09,132.09,129.9 4,129.94,129.00,129.00,128.13,122.69,113.87,113.87,85.67,84.81,83.37,82.6 4,80.50,80.44,77.25,61.56,59.22,58.39,57.95,56.15,55.56,53.95,50.40,49.26,49.11,44.00,41.93,39.81,39.20,35.72,35.01,29.82,26.38,21.85,21.75,13.60.

[0100] Example 59: Preparation of Compound 59 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of 4-fluorobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 51 F2NO9, pale yellow solid (110.3 mg), yield 74.6%. HRESIMS m / z:[(M+H) + ,740.35] 1 H NMR(400MHz,Chloroform-d)δ8.14(dd,J=8.8,5.4Hz,2H),8.00(dd,J=8.8,5.4Hz,2H),7.06(dt,J=24.0,8.6Hz,4H),5.25(d,J=5.4Hz,1H),4.15(t,J=7.4H) z,1H),4.02(d,J=6.0Hz,1H),3.64(d,J=8.2Hz,1H),3.47(d,J=9.0Hz,1H),3. 41-3.36(m,1H),3.31(s,3H),3.29(s,3H),3.27(s,3H),3.24(s,3H),3.19(dd ,J=8.4,7.0Hz,1H),3.08(d,J=8.4Hz,1H),3.03(dd,J=9.8,6.4Hz,1H),2.90( s,1H),2.54(dt,J=11.8,4.2Hz,2H),2.50-2.43(m,2H),2.40(s,1H),2.35(d, J=6.8Hz,2H),2.10(t,J=6.2Hz,3H),1.91(dq,J=10.8,4.6Hz,1H),1.82(s,1H ),1.64(dt,J=10.2,5.2Hz,2H),1.10(t,J=7.2Hz,3H),0.63(t,J=6.8Hz,3H). 13C NMR(100MHz,CDCl3)δ167.00,165.71,164.86,164.54,132.65,132.56,132.50,13 2.40,127.19,127.10,115.57,115.51,115.36,115.29,85.24,83.59,83.24,80.52 ,80.26,78.16,77.89,61.08,59.15,58.89,58.20,56.22,56.07,54.02,50.86,49.13,49.01,48.27,45.25,42.26,39.16,37.67,36.24,35.14,26.44,15.44,13.64.

[0101] Example 60: Preparation of Compound 60 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of 4-fluorobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was evaporated by rotation, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 42 H 54 FNO 10 Pale yellow solid (79.7 mg), yield 66.8%.

[0102] HRESIMS m / z:[(M+H) + ,752.37] 1H NMR(400MHz,Chloroform-d)δ8.07(d,J=8.8Hz,2H),8.00(dd,J=8.8,5.4Hz,2H),7.02(t,J=8.8Hz,2H),6.90(d,J=8.8Hz,2H),5.25(d,J=5.2Hz,1H), 4.13(dd,J=8.6,6.6Hz,1H),4.03(dd,J=6.4,1.6Hz,1H),3.84(s,3H),3.64 (d,J=8.2Hz,1H),3.53-3.42(m,1H),3.38(dd,J=8.0,6.6Hz,1H),3.31(s,3 H),3.29(s,3H),3.27(s,3H),3.24(s,3H),3.08(d,J=8.2Hz,1H),3.03(dd ,J=9.6,6.2Hz,1H),2.89(s,1H),2.68-2.63(m,1H),2.56-2.50(m,2H),2.5 0-2.43(m,2H),2.40-2.32(m,3H),2.11-2.06(m,3H),1.97-1.84(m,2H),1. 68-1.60(m,2H),1.36(s,1H),1.10(t,J=7.2Hz,3H),0.64(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ166.43,164.87,164.42,163.27,132.49,132.40,132.07,132. 07,127.23,123.26,115.45,115.23,113.54,113.54,85.18,83.53,83.23,80.53,80 .24,78.11,77.48,60.99,59.13,58.83,58.13,56.23,56.03,55.47,54.05,50.83,49.01,48.96,48.13,45.22,42.23,39.10,37.64,36.24,35.04,26.41,15.45,13.62.

[0103] Example 61: Preparation of Compound 61 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of 4-fluorobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 42 H 52 FNO 11 Pale yellow solid (80.8 mg), yield 68.1%. HRESIMS m / z:[(M+H) + ,766.35] 1 H NMR(400MHz,Chloroform-d)δ8.05(d,J=8.8Hz,2H),7.98(dd,J=8.8,5.4Hz,2H),7.02(t,J=8.8Hz,2H),6.90(d,J=8.8Hz,2H),5.26(d,J=5.2Hz,1H),4.13(dd ,J=8.8,5.8Hz,1H),3.98(d,J=6.6Hz,1H),3.83(s,3H),3.62(d,J=8.4Hz,1H), 3.53(dd,J=13.4,3.6Hz,1H),3.30(s,3H),3.26(s,3H),3.24(s,3H),3.15(s,3H) ),3.13(d,J=8.4Hz,1H),3.02(q,J=6.8,5.2Hz,3H),2.88(dd,J=7.2,5.2Hz,1H ),2.61-2.54(m,1H),2.54-2.48(m,2H),2.45(dt,J=12.0,3.8Hz,2H),2.33-2. 25(m,1H),2.11(d,J=1.8Hz,1H),2.10-2.05(m,1H),2.02-1.96(m,1H),1.96-1 .89(m,1H),1.65-1.57(m,2H),1.35(s,3H),1.26(s,1H),1.09(t,J=7.2Hz,3H). 13C NMR(100MHz,CDCl3)δ169.94,166.28,164.75,163.60,132.47,132.38,132.03,132. 03,127.02,122.55,115.48,115.26,113.87,113.87,85.57,84.80,83.32,82.93,80 .43,80.29,77.11,61.61,59.17,58.29,57.93,56.10,55.52,53.85,50.37,49.23,49.11,49.01,43.98,41.84,39.75,39.17,35.67,35.01,26.35,22.75,21.80,13.56.

[0104] Example 62: Preparation of Compound 62 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of m-methylbenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 43 H 57 NO9, pale yellow solid (97.0 mg), yield 66.3%. HRESIMS m / z:[(M+H) + ,732.40] 1H NMR(400MHz,Chloroform-d)δ7.97-7.91(m,2H),7.80(d,J=8.2Hz,2H),7.36-7.22(m,4H),5.29(d,J=5.2Hz,1H),4.18(dd,J=8.8,6.2Hz,1H),4.0 4(d,J=8.2Hz,1H),3.64(d,J=8.4Hz,1H),3.52-3.42(m,1H),3.40-3.35( m,1H),3.33(s,3H),3.30(s,3H),3.27(s,3H),3.24(s,3H),3.23-3.17(m ,1H),3.09(d,J=8.2Hz,1H),3.04(dd,J=9.8,6.2Hz,1H),2.92(s,1H),2. 67(t,J=6.4Hz,1H),2.59-2.52(m,2H),2.52-2.44(m,2H),2.44-2.39(m, 2H),2.38(s,3H),2.34(s,3H),2.11(q,J=6.4,5.8Hz,3H),1.90(dd,J=12 .8,6.8Hz,3H),1.64(s,2H),1.11(t,J=7.2Hz,3H),0.62(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ166.99,166.06,138.01,137.85,133.52,133.47,130.92,130.7 5,130.73,130.46,128.21,127.31,127.11,85.21,83.39,83.30,80.55,80.29,78.21 ,77.77,61.00,59.17,58.85,58.06,56.26,56.06,54.13,50.90,49.06,48.98,48.17,45.24,42.32,39.16,37.54,36.27,35.00,29.82,26.40,21.45,21.36,15.33,13.60.

[0105] Example 63: Preparation of Compound 63 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-ethylbenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 45 H 61 NO9, pale yellow solid (118.9 mg), yield 78.3%. HRESIMS m / z:[(M+H) + ,760.43] 1H NMR(400MHz,Chloroform-d)δ8.05(d,J=8.2Hz,2H),7.91(d,J=8.2Hz,2H),7.24(d,J=8.2 Hz,2H),7.19(d,J=8.2Hz,2H),5.26(d,J=5.2Hz,1H),4.20-4.09(m,1H),4.04(d,J=8.2Hz ,1H),3.64(d,J=8.2Hz,1H),3.47(q,J=11.6Hz,1H),3.40-3.34(m,1H),3.32(s,3H),3.30 (s,3H),3.27(s,3H),3.24(s,3H),3.22-3.17(m,1H),3.09(d,J=8.2Hz,1H),3.03(dd,J=9. 6,6.2Hz,1H),2.90(s,1H),2.67(dq,J=15.2,7.6Hz,5H),2.55(t,J=3.6Hz,1H),2.52(t,J =3.6Hz,1H),2.48(s,1H),2.45(d,J=4.8Hz,1H),2.39(s,1H),2.37(d,J=4.6Hz,1H),2.34 (d,J=5.6Hz,1H),2.09(d,J=8.6Hz,3H),1.89(dd,J=11.6,5.8Hz,1H),1.73(s,2H),1.64( s,1H),1.25-1.22(m,3H),1.22-1.18(m,3H),1.11(t,J=7.2Hz,3H),0.61(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ166.86,165.95,149.55,149.48,130.25,130.25,130.08,130.08,1 28.51,128.33,127.83,127.83,127.83,127.83,85.18,83.30,83.23,80.64,80.31,78.18 ,77.72,60.89,59.18,58.85,58.19,56.28,56.02,54.18,50.87,49.00,48.94,48.13,45.20,42.33,39.13,37.65,36.28,35.00,29.12,29.07,26.43,15.48,15.47,15.36,13.64.

[0106] Example 64: Preparation of Compound 64 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-bromobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 51 Br2NO9, pale yellow solid (160.2 mg), yield 93.2%. HRESIMS m / z:[(M+H) + ,860.19] 1 H NMR(400MHz,Chloroform-d)δ7.98(d,J=8.4Hz,2H),7.84(d,J=8.4Hz,2H),7.57(d,J=8.4Hz,2H),7.51(d,J=8.6Hz,2H),5.25(d,J=5.4Hz,1H),4.13(t,J=7) .4Hz,1H),4.02(d,J=6.6Hz,1H),3.65(d,J=8.2Hz,1H),3.51-3.42(m,1H),3. 42-3.36(m,1H),3.30(s,3H),3.29(s,3H),3.27(s,3H),3.24(s,3H),3.21-3. 15(m,1H),3.07(d,J=8.4Hz,1H),3.03(dd,J=9.8,6.2Hz,1H),2.88(s,1H),2. 66(t,J=5.2Hz,1H),2.57-2.53(m,1H),2.51(s,1H),2.49(s,1H),2.46(s,1H) ,2.40(s,1H),2.36-2.31(m,2H),2.10(t,J=6.6Hz,3H),1.91(dd,J=11.8,5.8 Hz,1H),1.65(d,J=18.6Hz,3H),1.10(t,J=7.2Hz,3H),0.64(t,J=6.8Hz,3H). 13C NMR(100MHz,CDCl3)δ165.94,165.11,131.73,131.73,131.66,131.66,131.63,13 1.63,131.50,131.50,129.83,129.71,127.98,127.86,85.24,83.75,83.20,80.35 ,80.24,78.16,77.95,61.14,59.18,58.93,58.17,56.27,56.12,53.98,50.85,49.11,49.05,48.23,45.21,42.24,39.16,37.66,36.14,35.16,26.44,15.56,13.66.

[0107] Example 65: Preparation of Compound 65 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-chlorobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 51 Cl2NO9, pale yellow solid (129.9 mg), yield 84.2%. HRESIMS m / z:[(M+H) + ,772.29] 1H NMR(400MHz,Chloroform-d)δ8.06(d,J=8.6Hz,2H),7.92(d,J=8.6Hz,2H),7.40(d ,J=8.6Hz,2H),7.34(d,J=8.6Hz,2H),5.25(d,J=5.2Hz,1H),4.17-4.11(m,1H),4.0 2(dd,J=6.6,1.6Hz,1H),3.65(d,J=8.2Hz,1H),3.52-3.42(m,1H),3.42-3.36(m,1H ),3.30(s,3H),3.29(s,3H),3.27(s,3H),3.24(s,3H),3.18(dd,J=8.2,6.8Hz,1H), 3.07(d,J=8.2Hz,1H),3.03(dd,J=9.8,6.2Hz,1H),2.89(s,1H),2.69-2.64(m,1H) ,2.57-2.50(m,2H),2.48(d,J=3.0Hz,1H),2.45(d,J=4.8Hz,1H),2.40(d,J=1.6Hz, 1H),2.34(tt,J=7.8,3.8Hz,3H),2.10(t,J=6.4Hz,3H),1.91(dt,J=11.6,5.2Hz,1H ),1.79(s,1H),1.63(d,J=4.8Hz,1H),1.10(t,J=7.2Hz,3H),0.64(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ165.79,164.94,139.25,139.15,131.48,131.48,131.34,13 1.34,129.39,129.26,128.71,128.71,128.64,128.64,85.21,83.71,83.20,80.39 ,80.23,78.14,77.93,61.11,59.16,58.92,58.17,56.25,56.09,53.98,50.84,49.10,49.02,48.21,45.21,42.23,39.15,37.66,36.16,35.15,26.43,15.53,13.66.

[0108] Example 66: Preparation of Compound 66 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of o-methoxybenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 43 H 57 NO 11 Pale yellow solid (127.5 mg), yield 83.5%. HRESIMS m / z:[(M+H) + ,764.39] 1 H NMR(400MHz,Chloroform-d)δ8.08(dd,J=8.0,1.8Hz,1H),7.81(dd,J=7.8,1.8Hz,1H ),7.42(dddd,J=21.6,8.4,7.4,1.8Hz,2H),6.98-6.88(m,4H),5.22(d,J=5.2Hz,1H), 4.17-4.11(m,1H),4.05(d,J=5.4Hz,1H),3.91(s,3H),3.84(s,3H),3.63(d,J=8.4Hz ,1H),3.51-3.45(m,1H),3.42-3.37(m,1H),3.36(s,3H),3.30(s,3H),3.27(s,3H),3. 25(s,3H),3.22(d,J=8.0Hz,1H),3.10(d,J=8.4Hz,1H),3.04(dd,J=9.4,6.2Hz,1H), 2.90(s,1H),2.69(dd,J=7.4,5.4Hz,1H),2.56(d,J=10.6Hz,1H),2.52-2.47(m,1H),2 .47-2.41(m,2H),2.39(d,J=1.8Hz,1H),2.32(dd,J=14.2,8.6Hz,2H),2.10(s,1H),1. 87(dd,J=12.2,6.0Hz,1H),1.66(s,5H),1.10(t,J=7.2Hz,3H),0.71(t,J=6.8Hz,3H). 13 C NMR(100MHz,CDCl3)δ165.25,165.15,160.23,159.61,133.74,133.26,133.26,132.3 8,120.91,120.17,120.08,119.66,112.25,111.94,84.98,83.41,83.16,80.69,80.35 ,78.31,78.31,60.37,59.19,58.83,58.24,56.22,56.17,55.98,54.49,50.91,48.83,48.73,47.96,45.03,42.40,39.11,37.49,36.26,34.79,29.83,26.39,15.45,13.58.

[0109] Example 67: Preparation of Compound 67 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of o-bromobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 51 Br2NO9, pale yellow solid (122.5 mg), yield 71.3%. HRESIMS m / z:[(M+H) + ,860.19] 1H NMR(400MHz,Chloroform-d)δ8.14(dd,J=7.6,2.2Hz,1H),7.81(dd,J=7.4,2.0Hz,1H),7.65( dd,J=7.8,1.4Hz,1H),7.59(dd,J=7.8,1.4Hz,1H),7.35-7.25(m,4H),5.26(d,J=5.2Hz,1H), 4.19-4.13(m,1H),4.04(d,J=5.6Hz,1H),3.63(d,J=8.4Hz,1H),3.53(dd,J=14.6,4.8Hz,1H) ,3.47-3.39(m,1H),3.36(s,3H),3.30(s,3H),3.29(s,3H),3.25(s,3H),3.22(d,J=8.4Hz,1H ),3.09(d,J=8.4Hz,1H),3.05(dd,J=9.8,6.4Hz,1H),2.89(s,1H),2.70(t,J=6.0Hz,1H),2.5 7-2.49(m,2H),2.47(d,J=3.6Hz,1H),2.45(d,J=4.8Hz,1H),2.41(d,J=6.8Hz,1H),2.34(dd, J=7.8,5.2Hz,2H),2.18(d,J=12.4Hz,1H),2.13-2.07(m,2H),1.90(td,J=11.4,10.8,4.4Hz, 1H),1.75(s,1H),1.64(td,J=10.8,5.4Hz,2H),1.10(t,J=7.2Hz,3H),0.76(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ165.23,164.85,134.76,134.26,133.05,132.84,132.60,13 2.39,131.91,130.76,127.18,127.11,123.06,121.90,85.17,84.00,83.25,80.23 ,78.19,77.89,60.89,59.15,58.91,58.21,56.18,56.12,54.09,53.55,50.87,49.08,48.95,48.20,45.22,42.23,39.15,37.54,36.14,35.07,26.45,15.58,13.64.

[0110] Example 68: Preparation of Compound 68 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of o-chlorobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 51 Cl2NO9, pale yellow solid (104.7 mg), yield 67.9%. HRESIMS m / z:[(M+H) + ,772.29] 1 H NMR(400MHz,Chloroform-d)δ8.13(dd,J=7.8,1.8Hz,1H),7.82(dd,J=7.8,1.8H z,1H),7.45-7.31(m,4H),7.29(ddd,J=7.8,7.2,1.6Hz,1H),7.23(dd,J=7.2,1.4 Hz,1H),5.28(s,1H),5.25(d,J=5.4Hz,1H),4.18-4.12(m,1H),4.04(d,J=5.4Hz, 1H),3.64(d,J=8.4Hz,1H),3.56-3.49(m,1H),3.46-3.38(m,1H),3.35(s,3H),3. 30(s,3H),3.29(s,3H),3.25(s,3H),3.09(d,J=8.2Hz,1H),3.05(dd,J=9.8,6.4 Hz,1H),2.89(s,1H),2.72-2.67(m,1H),2.58-2.49(m,2H),2.49-2.42(m,2H),2. 40(s,1H),2.38-2.28(m,3H),2.13-2.08(m,2H),1.94-1.86(m,1H),1.78(s,1H), 1.64(td,J=11.4,10.6,5.4Hz,2H),1.09(t,J=7.2Hz,3H),0.75(t,J=6.8Hz,3H). 13C NMR(100MHz,CDCl3)δ164.72,164.47,134.97,133.84,132.94,132.76,132.32,13 1.88,131.33,130.96,130.68,129.12,126.57,126.50,85.11,83.93,83.26,80.24 ,78.20,77.83,60.80,59.14,58.89,58.16,56.15,56.10,54.12,53.55,50.86,49.04,48.90,48.17,45.17,42.24,39.14,37.53,36.13,35.03,26.44,15.52,13.62.

[0111] Example 69: Preparation of Compound 69 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of o-fluorobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 51 F2NO9, pale yellow solid (101.1 mg), yield 68.4%. HRESIMS m / z:[(M+H) + ,740.35] 1H NMR(400MHz,Chloroform-d)δ8.08(td,J=7.6,1.8Hz,1H),7.89(td,J=7.6,1.8Hz,1H),7.53-7.41(m,2H),7.20-7.03(m,4H),5.27(d,J=5.2Hz,1H), 4.17-4.11(m,1H),4.04(d,J=6.4Hz,1H),3.64(d,J=8.2Hz,1H),3.57-3.4 7(m,1H),3.45-3.36(m,1H),3.34(s,3H),3.30(s,3H),3.28(s,3H),3.25( s,3H),3.08(d,J=8.4Hz,1H),3.04(dd,J=9.6,6.2Hz,1H),2.89(s,1H),2. 70(t,J=5.4Hz,1H),2.57-2.50(m,2H),2.48-2.43(m,2H),2.43-2.38(m,2 H),2.36-2.31(m,1H),2.17-2.05(m,3H),1.94-1.85(m,1H),1.73(s,2H), 1.65(dd,J=12.8,4.4Hz,2H),1.10(t,J=7.2Hz,3H),0.70(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ163.62,163.20,161.16,160.82,134.31,134.02,132.77,13 2.32,123.79,123.79,119.41,118.88,116.92,116.70,84.96,83.59,83.18,80.28 ,80.15,78.14,77.76,60.60,59.06,58.78,57.98,56.13,55.94,54.09,50.74,48.76,47.94,44.93,42.08,39.00,37.21,36.12,34.86,26.31,22.69,15.32,13.50.

[0112] Example 70: Preparation of Compound 70 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of m-bromobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 51 Br2NO9, pale yellow solid (122.9 mg), yield 71.5%.

[0113] HRESIMS m / z:[(M+H) + ,860.19] 1H NMR(400MHz,Chloroform-d)δ8.29(t,J=1.8Hz,1H),8.12(t,J=1.8Hz,1H),8.06(dt,J=7 .8,1.2Hz,1H),7.92(dt,J=7.8,1.2Hz,1H),7.64(dddd,J=14.2,8.0,2.0,1.2Hz,2H),7. 31(t,J=7.8Hz,1H),7.28-7.24(m,1H),5.29(d,J=5.2Hz,1H),4.17(t,J=7.2Hz,1H),4.0 2(dd,J=6.6,1.4Hz,1H),3.65(d,J=8.2Hz,1H),3.50-3.43(m,1H),3.42-3.36(m,1H),3. 32(s,3H),3.30(s,3H),3.28(s,3H),3.24(s,3H),3.07(d,J=8.2Hz,1H),3.03(dd,J=9.8 ,6.2Hz,1H),2.90(s,1H),2.66(dt,J=7.2,3.4Hz,1H),2.57-2.50(m,2H),2.50-2.43(m, 2H),2.42(s,1H),2.37(d,J=7.4Hz,2H),2.14-2.07(m,3H),1.92(dd,J=11.8,6.2Hz,1H) ,1.70(d,J=2.2Hz,3H),1.65-1.60(m,1H),1.11(t,J=7.2Hz,3H),0.66(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ165.35,164.48,135.76,135.74,133.37,132.94,132.85,13 2.74,129.95,129.95,128.63,128.53,122.44,122.39,85.28,84.02,83.19,80.24 ,80.14,78.16,77.92,61.22,59.17,58.93,57.98,56.27,56.18,53.94,50.86,49.14,49.07,48.27,45.32,42.25,39.18,37.46,36.11,35.22,26.43,15.47,13.67.

[0114] Example 71: Preparation of Compound 71 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of m-chlorobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 51 Cl2NO9, pale yellow solid (114.0 mg), yield 73.9%. HRESIMS m / z:[(M+H) + ,772.29] 1 H NMR(400MHz,Chloroform-d)δ8.13(t,J=1.8Hz,1H),8.01(dt,J=7.8,1.4Hz,1H),7.97( t,J=1.8Hz,1H),7.87(dt,J=7.8,1.4Hz,1H),7.48(dddd,J=15.2,8.0,2.2,1.2Hz,2H), 7.34(dt,J=21.8,7.8Hz,2H),5.29(s,1H),4.16(t,J=7.4Hz,1H),4.02(d,J=8.4Hz,1H) ,3.65(d,J=8.2Hz,1H),3.51-3.44(m,1H),3.39(dd,J=14.6,7.6Hz,1H),3.31(s,3H),3. 30(s,3H),3.28(s,3H),3.23(s,3H),3.20(d,J=6.8Hz,1H),3.07(d,J=8.2Hz,1H),3.03 (dd,J=9.8,6.2Hz,1H),2.90(s,1H),2.66(t,J=5.2Hz,1H),2.57-2.50(m,2H),2.48(d, J=4.4Hz,1H),2.47-2.40(m,2H),2.37(d,J=7.4Hz,2H),2.10(t,J=7.0Hz,3H),1.97-1. 87(m,1H),1.78(s,1H),1.68-1.58(m,2H),1.10(t,J=7.2Hz,3H),0.66(t,J=6.8Hz,3H). 13 C NMR(100MHz,CDCl3)δ165.32,164.48,134.34,134.30,132.72,132.67,132.59,13 2.48,130.25,129.90,129.55,129.55,128.07,127.94,85.15,83.89,83.10,80.14 ,80.10,78.05,77.82,61.08,59.04,58.80,57.88,56.09,56.03,53.84,53.44,50.75,48.93,48.23,45.22,42.15,39.08,37.36,36.02,35.10,26.32,15.32,13.54.

[0115] Example 72: Preparation of Compound 72 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of m-fluorobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 51 F2NO9, pale yellow solid (121.4 mg), yield 82.1%. HRESIMS m / z:[(M+H) + ,740.35] 1H NMR(400MHz,Chloroform-d)δ7.92(dt,J=7.8,1.2Hz,1H),7.82(ddd,J=9.6,2.6,1.4Hz,1H) ,7.78(dt,J=7.8,1.2Hz,1H),7.67(ddd,J=9.4,2.8,1.4Hz,1H),7.38(dtd,J=22.8,8.0,5.4 Hz,2H),7.26-7.16(m,2H),5.27(d,J=5.2Hz,1H),4.16(t,J=7.4Hz,1H),4.02(dd,J=6.6,1. 6Hz,1H),3.65(d,J=8.2Hz,1H),3.52-3.43(m,1H),3.43-3.35(m,1H),3.31(s,3H),3.30(s, 3H),3.28(s,3H),3.24(s,3H),3.21(dd,J=8.2,6.8Hz,1H),3.07(d,J=8.2Hz,1H),3.03(dd, J=9.8,6.2Hz,1H),2.90(s,1H),2.67(td,J=5.8,1.6Hz,1H),2.57-2.53(m,1H),2.52(s,1H) ,2.48(d,J=3.6Hz,1H),2.45(d,J=5.0Hz,1H),2.41(s,1H),2.36(d,J=7.4Hz,3H),2.14-2.0 5(m,3H),1.96-1.87(m,1H),1.69-1.57(m,2H),1.10(t,J=7.2Hz,3H),0.64(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ165.52,164.69,163.81,161.36,133.13,133.00,130.00,12 9.93,125.83,125.66,120.02,119.81,117.12,116.89,85.24,83.84,83.19,80.29 ,80.23,78.15,77.97,61.14,59.16,58.91,58.11,56.24,56.12,53.96,50.84,49.11,49.03,48.24,45.23,42.22,39.15,37.59,36.13,35.17,26.43,15.38,13.65.

[0116] Example 73: Preparation of Compound 73 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of 2,4-dichlorobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 49 Cl4NO9, pale yellow solid (144.5 mg), yield 86.1%. HRESIMS m / z:[(M+H) + ,840.21] 1 H NMR(400MHz,Chloroform-d)δ8.08(d,J=8.4Hz,1H),7.77(d,J=8.4Hz,1H),7.46(d,J =2.0Hz,1H),7.41(d,J=2.2Hz,1H),7.29(dd,J=8.4,2.2Hz,1H),7.23(dd,J=8.4,2.0 Hz,1H),5.23(d,J=5.2Hz,1H),4.12(dd,J=8.8,6.2Hz,1H),4.05-4.00(m,1H),3.64( d,J=8.2Hz,1H),3.50(d,J=10.4Hz,1H),3.43(dd,J=8.2,6.8Hz,1H),3.31(s,3H),3.3 0(s,3H),3.29(s,3H),3.24(s,3H),3.07(d,J=8.4Hz,1H),3.05-3.00(m,1H),2.87(s ,1H),2.67(t,J=6.2Hz,1H),2.53(t,J=8.8Hz,2H),2.47(dd,J=10.2,6.8Hz,2H),2.40 (s,1H),2.35(dd,J=14.4,8.8Hz,2H),2.26(dd,J=14.4,6.2Hz,1H),2.17-2.05(m,3H ),1.95-1.86(m,1H),1.69-1.57(m,2H),1.09(t,J=7.2Hz,3H),0.78(t,J=6.8Hz,3H). 13 C NMR(100MHz,CDCl3)δ163.81,163.58,138.55,138.07,136.05,135.02,133.85,13 2.93,131.22,130.90,128.92,127.50,127.01,127.01,85.12,84.21,83.19,80.20 ,80.06,78.17,77.85,60.89,59.15,58.95,58.12,56.14,54.04,54.04,50.84,49.10,48.94,48.20,45.18,42.21,39.14,37.54,36.04,35.12,26.43,15.68,13.63.

[0117] Example 74: Preparation of Compound 74 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of 3,5-difluorobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 49 F4NO9, pale yellow solid (137.2 mg), yield 88.5%. HRESIMS m / z:[(M+H) + ,776.33] 1H NMR(400MHz,Chloroform-d)δ7.65(dd,J=7.8,2.4Hz,2H),7.50(dd,J=7.8,2.4Hz,2H),6.97(dtt,J=14.8,8.4,2.4Hz,2H),5.26(d,J=5.2Hz,1H),4.14(dd, J=8.8,5.6Hz,1H),4.01(dd,J=6.4,1.6Hz,1H),3.66(d,J=8.2Hz,1H),3.50-3 .38(m,2H),3.30(s,3H),3.30(s,3H),3.28(s,3H),3.24(s,3H),3.08-3.04(m, 1H),3.04-3.00(m,1H),2.89(s,1H),2.66(t,J=6.2Hz,1H),2.55(dd,J=7.0,4 .8Hz,1H),2.53-2.51(m,1H),2.49(d,J=6.2Hz,1H),2.47-2.44(m,1H),2.44-2 .40(m,1H),2.40-2.29(m,3H),2.14-2.07(m,3H),1.96-1.89(m,1H),1.67(s, 2H),1.63(td,J=5.6,2.4Hz,1H),1.10(t,J=7.2Hz,3H),0.70(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ164.37,164.12,164.00,163.59,161.63,161.52,134.15,13 4.09,113.27,113.09,113.01,112.83,108.32,108.24,85.30,84.34,83.17,80.23 ,80.06,78.15,78.15,61.31,59.17,58.98,58.04,56.21,56.21,53.88,50.87,49.25,49.11,48.39,45.34,42.22,39.22,37.53,36.03,35.30,26.45,15.46,13.67.

[0118] Example 75: Preparation of Compound 75 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of o-methylbenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 43 H 57 NO9, pale yellow solid (128.1 mg), yield 87.6%. HRESIMS m / z:[(M+H) + ,732.40] 1 H NMR(400MHz,Chloroform-d)δ8.12(dd,J=8.2,1.4Hz,1H),7.87(dd,J=8.2,1.4Hz,1 H),7.42-7.29(m,2H),7.25-7.15(m,4H),5.19(d,J=5.2Hz,1H),4.15(t,J=7.6Hz,1 H),4.06(dd,J=6.4,1.4Hz,1H),3.64(d,J=8.2Hz,1H),3.53(d,J=9.8Hz,1H),3.43- 3.34(m,1H),3.33(s,3H),3.31(s,3H),3.29(s,3H),3.26(s,3H),3.21-3.15(m,1H) ,3.10(d,J=8.2Hz,1H),3.05(dd,J=9.8,6.2Hz,1H),2.90(s,1H),2.69(dd,J=5.8,3 .4Hz,1H),2.66(s,3H),2.55(s,3H),2.53(d,J=4.6Hz,1H),2.39(d,J=1.4Hz,1H),2 .33(dd,J=7.8,2.6Hz,3H),2.10(dt,J=5.8,3.8Hz,3H),1.90(dd,J=11.2,5.6Hz,1H ),1.74(s,3H),1.62(d,J=7.8Hz,2H),1.10(t,J=7.2Hz,3H),0.68(t,J=6.8Hz,3H). 13C NMR(100MHz,CDCl3)δ167.25,167.23,141.00,139.92,131.93,131.64,131.64,131.5 7,131.49,130.96,130.80,129.63,125.70,125.68,85.24,83.35,83.30,80.30,80.30 ,78.21,78.21,61.00,59.18,58.88,57.97,56.24,56.03,54.13,50.90,49.08,49.01,48.18,45.13,42.37,39.14,37.52,36.39,35.03,26.46,22.03,21.67,15.44,13.65.

[0119] Example 76: Preparation of Compound 76 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of o-methoxybenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 43 H 57 NO 11 Pale yellow solid (99.7 mg), yield 65.3%. HRESIMS m / z:[(M+H) + ,764.39] 1H NMR(400MHz,Chloroform-d)δ7.73(dt,J=7.8,1.2Hz,1H),7.70(dd,J=2.8,1.4Hz,1H),7.59(dt,J=7.8,1.2Hz,1H),7.52(dd,J=2.6,1.4Hz,1H),7.33(t,J=7.8Hz,1H),7.27(t,J=7.8Hz,1H),7.06(dddd,J=15.8,8.2,2.6,1.0Hz,2H),5.28(d,J=5.2Hz,1H),4.15(dd,J=8.6,6.4Hz,1H),4.04(dd,J=6.6,1.4Hz,1H),3.83(s,3H),3.78(s,3H),3.65(d,J=8.2Hz,1H),3.51-3.42(m,1H),3.38(dt,J=8.0,6.8Hz,1H),3.31(s,3H),3.30(s,3H),3.28(s,3H),3.25(s,3H),3.21(dd,J=8.2,6.8Hz,1H),3.08(d,J=8.2Hz,1H),3.04(dd,J=9.6,6.2Hz,1H),2.91(s,1H),2.70-2.65(m,1H),2.58-2.51(m,2H),2.50-2.43(m,2H),2.42-2.35(m,3H),2.11(dd,J=6.8,2.4Hz,2H),1.90(q,J=5.8Hz,1H),1.76(s,3H),1.65(dd,J=13.0,4.8Hz,1H),1.11(t,J=7.2Hz,3H),0.65(t,J=6.8Hz,3H). 13 C NMR(100MHz,CDCl3)δ166.53,165.74,159.49,159.49,132.31,132.09,129.35,129.33,122.61,122.41,119.67,119.51,114.20,114.05,85.21,83.59,83.25,80.51,80.26,78.17,77.81,60.94,59.17,58.88,58.18,56.29,56.11,55.46,55.44,54.13,50.87,49.04,48.95,48.14,45.19,42.33,39.13,37.67,36.11,35.05,26.41,15.42,13.62.

[0120] Example 77: Preparation of Compound 77 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent amounts of butyryl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 35 H 57 NO9, pale yellow solid (99.9 mg), yield 78.6%. HRESIMS m / z:[(M+H) + ,636.40] 1 H NMR(400MHz,Chloroform-d)δ4.85(d,J=5.2Hz,1H),3.97(dd,J=6.6,1.6Hz,1H),3.89(t,J=7.8Hz,1H),3.62(d,J=8.2Hz,1H),3.46(dt,J=8.8, 7.0Hz,1H),3.37-3.30(m,2H),3.28(d,J=1.8Hz,9H),3.19(s,3H),3.05 (d,J=8.2Hz,1H),2.97(dd,J=9.4,6.2Hz,1H),2.76(s,1H),2.48-2.45(m ,2H),2.43(t,J=3.6Hz,2H),2.40(s,1H),2.39-2.34(m,2H),2.26(dd,J=7.4,3.2Hz,3H),2.24(d,J=3.2Hz,1H),2.20(d,J=5.2Hz,1H),2.04(d, J=6.4Hz,1H),1.95(ddd,J=12.4,7.2,5.2Hz,1H),1.88-1.80(m,3H),1.62(dq,J=14.8,7.4Hz,6H),1.07(q,J=7.0Hz,6H),0.93(q,J=7.4Hz,6H). 13C NMR(100MHz,CDCl3)δ173.83,172.98,84.97,83.39,82.10,80.34,80.22,78.28,78.28,60.64,59.13,58.84,57.96,56.14,56.10,54.16 ,50.80,48.83,48.67,47.76,44.80,42.05,39.01,37.46,36.40,36.36,36.36,34.85,26.39,18.65,18.05,16.21,13.79,13.69,13.54.

[0121] Example 78: Preparation of Compound 78 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent amounts of butyryl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 39 H 57 NO 10 Pale yellow solid (64.3 mg), yield 57.9%. HRESIMS m / z:[(M+H) + ,700.39] 1H NMR(400MHz,Chloroform-d)δ8.03(d,J=8.8Hz,2H),6.90(d,J=8.8Hz,2H),5.02(d, J=5.2Hz,1H),4.03-3.97(m,2H),3.84(s,3H),3.61(d,J=8.2Hz,1H),3.35(s,3H),3 .30(d,J=6.8Hz,1H),3.28(s,3H),3.24(s,3H),3.22(s,3H),3.15-3.10(m,1H),3.0 7(d,J=8.2Hz,1H),3.00(dd,J=9.8,6.2Hz,1H),2.81(s,1H),2.63-2.58(m,1H),2.5 3-2.50(m,1H),2.48(t,J=3.6Hz,1H),2.44(d,J=2.2Hz,1H),2.43-2.39(m,1H),2.3 3(s,1H),2.31-2.28(m,2H),2.28-2.25(m,2H),2.25-2.22(m,1H),2.05(d,J=6.4Hz ,1H),2.00(dd,J=7.0,5.2Hz,1H),1.96-1.87(m,2H),1.61(p,J=7.2Hz,4H),1.38(d ,J=20.4Hz,1H),1.07(t,J=7.2Hz,3H),0.91(t,J=7.4Hz,3H),0.55(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ173.11,166.36,163.17,132.03,132.03,123.42,113.4 7,113.47,85.14,83.22,82.56,80.42,80.26,78.07,77.54,60.94,59.13,58 .79,58.00,56.16,55.91,55.47,54.06,50.78,48.94,48.91,48.10,44.98,42.19,39.08,37.51,36.50,36.22,34.98,26.41,18.68,15.36,13.67,13.60.

[0122] Example 79: Preparation of Compound 79 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent amounts of butyryl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was evaporated by rotation, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 39 H 55 NO 11 Pale yellow solid (58.7 mg), yield 53.1%. HRESIMS m / z:[(M+H) + ,714.37] 1 H NMR(400MHz,Chloroform-d)δ8.02(d,J=8.8Hz,2H),6.90(d,J=8.8Hz,2H),5.06(d,J=5.2Hz,1H),3.99(dd,J=8.8,5.8Hz,1H),3.94(d,J=6.6H) z,1H),3.84(s,3H),3.60(d,J=8.4Hz,1H),3.40(dd,J=15.6,5.8Hz,1H) ,3.34(s,3H),3.26(s,3H),3.22(s,3H),3.13(s,3H),3.11(s,1H),2.99 (q,J=6.0Hz,3H),2.94(s,1H),2.82(dd,J=7.2,5.4Hz,1H),2.57-2.48(m,1H),2.47-2.43(m,2H),2.42-2.39(m,1H),2.25(pd,J=8.0,3.2Hz,3 H),2.06(dd,J=11.2,6.6Hz,2H),1.97-1.87(m,3H),1.62-1.57(m,3H),1.28(s,3H),1.23(s,1H),1.07(t,J=7.2Hz,3H),0.91(t,J=7.4Hz,3H). 13C NMR(100MHz,CDCl3)δ173.02,169.95,166.23,163.52,132.02,132.02,122.6 9,113.82,113.82,85.63,84.78,83.29,82.00,80.45,80.12,77.12,61.58,5 9.19, 58.16, 57.91, 56.05, 55.54, 53.86, 50.32, 49.20, 49.09, 48.96, 43.81, 41.81, 39.66, 39.15, 36.43, 35.66, 34.97, 26.35, 21.77, 18.66, 13.66, 13.55.

[0123] Example 80: Preparation of Compound 80 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, twice the equivalent volume of isobutyryl chloride was added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 35 H 57 NO9, pale yellow solid (66.0 mg), yield 51.9%. HRESIMS m / z:[(M+H) + ,636.40] 1H NMR(400MHz,Chloroform-d)δ4.94(d,J=5.2Hz,1H),3.99(dd,J=6.8,1.6Hz,1H),3.84(t,J=7.8Hz,1H),3.64(d,J=8.2Hz,1H),3.48(dq,J=9.0,7.0Hz ,1H),3.35(dd,J=8.4,7.0Hz,1H),3.30(s,3H),3.29(s,3H),3.24(s,3H),3 .20(s,3H),3.04(d,J=8.2Hz,1H),2.98(dd,J=9.2,6.2Hz,1H),2.78(s,1H) ,2.59-2.54(m,1H),2.54-2.49(m,2H),2.49-2.43(m,2H),2.43-2.36(m,3H ),2.22(dd,J=8.0,2.2Hz,2H),2.06(d,J=6.4Hz,1H),1.97(ddd,J=12.2,7. 2,5.2Hz,1H),1.90-1.79(m,2H),1.75(d,J=3.2Hz,2H),1.62(tdd,J=13.4, 7.2,4.8Hz,2H),1.18(t,J=7.2Hz,6H),1.09(ddd,J=9.6,7.0,4.2Hz,12H). 13 C NMR (100MHz, CDCl3) δ176.84,176.34,84.86,83.52,82.05,80.26,80.10,78.30,76.70,60.37,59.16,58.82,57.82,56.15,56.07,54.38 ,50.89,48.74,48.49,47.52,45.15,42.33,38.99,37.40,36.06,34.72,34.38,34.21,26.33,19.19,19.13,19.05,18.77,16.16,13.52.

[0124] Example 81: Preparation of Compound 81 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, twice the equivalent volume of isobutyryl chloride was added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 39 H 57 NO 10 Pale yellow solid (57.5 mg), yield 51.8%. HRESIMS m / z:[(M+H) + ,700.39] 1 H NMR(400MHz,Chloroform-d)δ8.05(d,J=8.8Hz,2H),6.90(d,J=8.8Hz,2H),5.03(d,J=5.2Hz,1H),4.02-3.94(m,2H),3.85(s,3H),3.62(d,J=8.2Hz,1H) ,3.33(s,3H),3.31-3.29(m,1H),3.28(s,3H),3.25(s,3H),3.22(s,3H),3. 16-3.11(m,1H),3.07(d,J=8.2Hz,1H),3.01(dd,J=9.4,6.2Hz,1H),2.82(s, 1H),2.61(dd,J=7.2,5.4Hz,1H),2.55-2.46(m,3H),2.45-2.40(m,2H),2.3 4(d,J=1.5Hz,1H),2.28(dd,J=7.6,4.4Hz,2H),2.06(d,J=6.4Hz,1H),2.01( dd,J=7.0,5.2Hz,1H),1.94-1.82(m,3H),1.61(q,J=4.2Hz,2H),1.41(s,1H) ),1.11(dd,J=6.8,1.2Hz,6H),1.07(t,J=7.2Hz,3H),0.57(t,J=6.8Hz,3H). 13C NMR(100MHz,CDCl3)δ176.55,166.36,163.18,132.00,132.00,123.49,113.5 0,113.50,85.01,83.28,82.34,80.38,80.29,78.13,77.54,60.70,59.15,58 .81,58.01,56.12,55.95,55.49,54.23,50.79,48.88,48.82,48.02,44.98,42.29,39.07,37.56,36.09,34.90,34.08,26.39,19.18,19.16,15.43,13.58.

[0125] Example 82: Preparation of Compound 82 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, twice the equivalent volume of isobutyryl chloride was added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was evaporated by rotation, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 39 H 55 NO 11 Pale yellow solid (59.6 mg), yield 53.9%. HRESIMS m / z:[(M+H) + ,712.37] 1H NMR(400MHz,Chloroform-d)δ8.02(d,J=8.8Hz,2H),6.90(d,J=8.8Hz,2H),5.05(d,J=5.2Hz,1H),3.95(dd,J=8.2,6.2Hz,2H),3.84(s, 3H),3.60(d,J=8.4Hz,1H),3.38(dd,J=15.6,5.8Hz,1H),3.31(s,3H),3.25(s,3H),3.22(s,3H),3.13(s,3H),3.01-2.95(m,3H),2.94( s,1H),2.82(dd,J=7.2,5.4Hz,1H),2.56-2.46(m,3H),2.45-2.37(m,3H),2.25(tdd,J=12.2,7.2,3.8Hz,1H),2.06(dd,J=11.6,6.2Hz, 2H),1.95-1.85(m,3H),1.59(dt,J=12.6,4.2Hz,2H),1.30(s,3H),1.11(d,J=1.0Hz,3H),1.09(d,J=1.0Hz,3H),1.06(t,J=7.2Hz,3H). 13 C NMR (100MHz, CDCl3) δ176.44,169.94,166.21,163.50,131.96,131.96,122.7 2,113.82,113.82,85.66,84.64,83.31,81.74,80.45,80.05,77.10,61.38,5 9.18, 58.13, 57.89, 55.98, 55.52, 53.95, 50.31, 49.14, 48.98, 48.87, 43.77, 41.86, 39.66, 39.12, 35.52, 34.90, 34.01, 26.32, 21.77, 19.12, 19.12, 13.51.

[0126] Example 83: Preparation of Compound 83 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-chlorobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 42 H 54 ClNO 10 Pale yellow solid (57.8 mg), yield 47.4%. HRESIMS m / z:[(M+H) + ,768.34] 1H NMR(400MHz,Chloroform-d)δ8.07(d,J=8.6Hz,2H),7.92(d,J=8.6Hz,2H),7.34(d,J=8.6Hz,2H),6.91(d,J=8.8Hz,2H),5.25(d,J=5.2Hz,1H),4.12(dd,J=8.4,6.4Hz,1H),4.03(dd,J=6.4,1.4Hz,1H),3.85(s,3H),3.64(d,J=8.2Hz,1H),3.53-3.45(m,1H),3.42-3.34(m,1H),3.30(s,3H),3.30(s,3H),3.27(s,3H),3.24(s,3H),3.20(dt,J=8.2,6.8Hz,1H),3.08(d,J=8.2Hz,1H),3.03(dd,J=9.6,6.2Hz,1H),2.89(s,1H),2.66(dt,J=7.2,3.4Hz,1H),2.54(dd,J=7.2,4.8Hz,1H),2.51(d,J=1.6Hz,1H),2.49(d,J=5.4Hz,1H),2.45(dd,J=4.8,2.2Hz,1H),2.40(s,1H),2.36(dd,J=7.6,5.4Hz,2H),2.34-2.28(m,1H),2.10(s,1H),2.08(dd,J=4.2,1.6Hz,1H),1.90(dd,J=11.4,5.6Hz,1H),1.68(dd,J=13.2,4.2Hz,2H),1.64-1.61(m,1H),1.10(t,J=7.0Hz,3H),0.65(t,J=7.0Hz,3H). 13 C NMR(100MHz,CDCl3)δ166.46,165.00,163.31,139.06,132.10,132.10,131.38,131.38,129.50,128.61,128.61,123.29,113.58,113.58,85.21,83.71,83.27,80.50,80.28,78.13,77.48,61.05,59.18,58.87,58.14,56.27,56.06,55.52,54.07,50.86,49.05,49.00,48.18,45.24,42.26,39.14,37.65,36.22,35.07,26.45,15.49,13.66.

[0127] Example 84: Preparation of Compound 84 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-chlorobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 42 H 52 ClNO 11 Pale yellow solid (82.1 mg), yield 67.8%. HRESIMS m / z:[(M+H) + ,782.32] 1 H NMR(400MHz,Chloroform-d)δ8.04(d,J=8.8Hz,2H),7.90(d,J=8.6Hz,2H),7.3 2(d,J=8.6Hz,2H),6.90(d,J=8.8Hz,2H),5.26(d,J=5.2Hz,1H),4.11(dd,J=8. 8,5.8Hz,1H),3.98(d,J=6.8Hz,1H),3.83(s,3H),3.61(d,J=8.4Hz,1H),3.57- 3.50(m,1H),3.29(s,3H),3.26(s,3H),3.23(s,3H),3.15(s,3H),3.12(s,1H), 3.02(dd,J=10.4,6.8Hz,4H),2.88(dd,J=7.2,5.2Hz,1H),2.60-2.54(m,1H),2 .54-2.50(m,1H),2.48(d,J=3.8Hz,1H),2.46(q,J=3.2,2.2Hz,1H),2.45-2.40 (m,1H),2.33-2.23(m,1H),2.15-2.10(m,2H),2.08(d,J=7.0Hz,1H),1.95-1.8 8(m,1H),1.61(tq,J=8.2,4.8,4.2Hz,2H),1.34(s,3H),1.09(t,J=7.2Hz,3H). 13 C NMR(100MHz,CDCl3)δ169.90,166.24,164.82,163.58,139.10,132.01,132.01,131. 29,131.29,129.27,128.58,128.58,122.54,113.86,113.86,85.53,84.78,83.31,8 3.06, 80.42, 80.22, 77.05, 61.62, 59.17, 58.26, 57.92, 56.08, 55.52, 53.83, 53.54, 50.35, 49.26, 49.11, 43.96, 41.83, 39.72, 39.16, 35.61, 35.01, 26.36, 21.80, 13.57.

[0128] Example 85: Preparation of Compound 85 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of crotonyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 35 H 53 NO9, pale yellow solid (68.8 mg), yield 54.5%. HRESIMS m / z:[(M+H) + ,632.37] 1H NMR(400MHz,Chloroform-d)δ6.96-6.88(m,2H),5.88(dt,J=15.4,2.2Hz,2H), 5.85-5.79(m,1H),5.30(d,J=12.4Hz,1H),4.92(t,J=5.2Hz,1H),4.04-3.92(m ,2H),3.60(d,J=8.2Hz,1H),3.46-3.39(m,1H),3.32(s,3H),3.28(s,3H),3.27 (s,3H),3.23(s,3H),3.16-3.09(m,1H),3.09-3.02(m,2H),2.90(d,J=5.0Hz,1H ),2.75(d,J=10.4Hz,1H),2.70-2.61(m,2H),2.52(t,J=6.2Hz,1H),2.38(d,J= 1.8Hz,1H),2.25(d,J=7.8Hz,2H),2.14(td,J=4.8,2.2Hz,2H),2.07-1.98(m,2 H),1.98-1.91(m,1H),1.86(d,J=1.8Hz,1H),1.85(d,J=1.8Hz,2H),1.84-1.83 (m,2H),1.82(s,1H),1.69(s,2H),1.15(t,J=7.2Hz,3H),1.00(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ166.57,165.80,144.77,144.77,123.23,123.17,83.82,82.98,81.89,80.59,79.57,78.19,78.16,78.15,60.85,59. 16,58.86,58.28,56.21,56.08,54.76,50.87,49.01,48.87,46.02,4 4.35,41.74,38.77,37.56,36.19,25.26,18.03,18.03,15.90,12.65.

[0129] Example 86: Preparation of Compound 86 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of crotonyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 39 H 55 NO 10 Pale yellow solid (91.5 mg), yield 82.6%. HRESIMS m / z:[(M+H) + ,698.38] 1 H NMR(400MHz,Chloroform-d)δ8.04(dd,J=9.0,2.2Hz,2H),6.89(d,J=8.8Hz,3H) ,5.90-5.76(m,1H),5.08(dd,J=8.2,5.2Hz,1H),4.06-3.98(m,2H),3.84(s,3H) ,3.61(d,J=8.2Hz,1H),3.37(s,1H),3.35(s,3H),3.34-3.30(m,1H),3.28(s,3H) ),3.24(s,3H),3.23(s,3H),3.19-3.10(m,1H),3.07(d,J=8.6Hz,1H),3.05-3.0 0(m,1H),2.87(s,1H),2.61(t,J=6.2Hz,1H),2.59-2.51(m,4H),2.35(d,J=7.8H z,2H),2.32(d,J=2.6Hz,1H),2.29(s,1H),2.28-2.22(m,1H),2.09(d,J=6.4Hz, 1H),2.03(ddd,J=6.2,4.2,1.8Hz,2H),1.86-1.83(m,1H),1.81(dd,J=6.8,1.6H z,3H),1.64(dd,J=9.0,4.8Hz,2H),1.10(t,J=7.2Hz,3H),0.57(t,J=6.8Hz,3H). 13C NMR(100MHz,CDCl3)δ166.42,165.83,163.23,144.43,132.10,132.04,123.4 2,123.28,113.50,113.50,84.79,83.14,82.49,80.67,80.06,78.08,77.55,6 1.03, 59.15, 58.83, 58.25, 56.20, 56.00, 55.49, 54.24, 50.83, 49.00, 48.96, 47.52, 44.92, 42.09, 39.02, 37.60, 36.23, 34.31, 26.06, 18.02, 15.34, 13.33.

[0130] Example 87: Preparation of Compound 87 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalent volumes of crotonyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 39 H 53 NO 11 Pale yellow solid (54.6 mg), yield 49.5%. HRESIMS m / z:[(M+H) + ,712.36] 1H NMR(400MHz,Chloroform-d)δ8.03(d,J=9.2Hz,2H),6.96-6.86(m,3H),5.88-5.79(m,2H),5.13(d,J=5.2Hz,1H),4.03(dd,J=8.8,5.8Hz,1H), 3.96(d,J=6.8Hz,1H),3.84(s,3H),3.61(d,J=8.4Hz,1H),3.35(s,3H) ,3.27(s,3H),3.24(s,3H),3.14(s,3H),3.12(s,1H),3.05-3.02(m,1H) ,3.02-2.98(m,3H),2.84(dd,J=7.2,5.4Hz,1H),2.54(s,3H),2.46(dd,J=15.8,5.8Hz,1H),2.29-2.19(m,1H),2.12(d,J=6.7Hz,1H),2.04-1. 96(m,1H),1.88(dq,J=6.8,1.6Hz,3H),1.81(dd,J=6.8,1.6Hz,3H),1.68-1.62(m,1H),1.62-1.54(m,1H),1.30(s,3H),1.11(t,J=7.2Hz,3H). 13 C NMR (100MHz, CDCl3) δ170.02,166.30,165.75,163.59,144.74,132.10,132.1 0,123.21,122.57,113.86,113.86,85.50,84.47,83.24,81.96,80.38,80.28, 77.16,61.63,59.22,58.42,57.98,56.11,55.56,54.05,50.40,49.21,48.97,48.65,43.77,41.72,39.75,39.11,35.69,34.36,26.03,21.76,18.04,13.30.

[0131] Example 88: Preparation of Compound 88 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of 3,3-dimethylbutyryl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 39 H 65 NO9, pale yellow solid (75.5 mg), yield 54.6%. HRESIMS m / z:[(M+H) + ,692.46] 1 H NMR(400MHz,Chloroform-d)δ4.85(d,J=5.2Hz,1H),3.98(dd,J=6.4,1.8Hz,1H),3.89(t,J=7.8Hz,1H),3.63(d,J=8.2Hz,1H),3.50-3.43(m,1H),3.37-3 .31(m,2H),3.29(s,6H),3.26(s,3H),3.20(s,3H),3.06(d,J=8.2Hz,1H),2. 98(dd,J=9.4,6.2Hz,1H),2.77(s,1H),2.52-2.48(m,1H),2.47-2.43(m,2H), 2.40(d,J=4.6Hz,1H),2.36(d,J=1.6Hz,1H),2.29(s,1H),2.25(s,1H),2.20 (t,J=8.2Hz,2H),2.17(s,1H),2.15-2.13(m,2H),2.04(d,J=6.4Hz,1H),1.9 3(dd,J=7.2,5.2Hz,1H),1.88-1.79(m,2H),1.76-1.71(m,1H),1.65-1.57(m ,2H),1.09(t,J=6.8Hz,3H),1.06(t,J=7.2Hz,3H),1.03(s,9H),1.01(s,9H). 13C NMR(100MHz,CDCl3)δ172.52,171.62,85.01,83.43,82.20,80.26,80.13,7 8.20,77.03,60.63,59.15,58.84,57.55,56.13,56.06,54.20,50.83,48.85 ,48.74,48.42,48.12,47.80,44.88,42.20,39.03,37.44,36.37,34.87,30.89,30.49,29.77,29.77,29.77,29.74,29.74,29.74,26.43,16.35,13.58.

[0132] Example 89: Preparation of Compound 89 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of 3,3-dimethylbutyryl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 61 NO 10 Pale yellow solid (83.1 mg), yield 71.9%. HRESIMS m / z:[(M+H) + ,728.42] 1H NMR(400MHz,Chloroform-d)δ8.03(d,J=8.8Hz,2H),6.90(d,J=8.8Hz,2H),5.0 2(d,J=5.2Hz,1H),4.06-3.97(m,2H),3.85(s,3H),3.62(d,J=8.2Hz,1H),3.36( s,3H),3.32(dd,J=8.2,6.4Hz,2H),3.28(s,3H),3.25(s,3H),3.22(s,3H),3.13 (dd,J=8.2,6.8Hz,1H),3.07(d,J=8.2Hz,1H),3.00(dd,J=9.6,6.2Hz,1H),2.82 (s,1H),2.62(dd,J=7.0,5.4Hz,1H),2.53-2.47(m,2H),2.44(dd,J=11.4,4.8Hz ,2H),2.34(d,J=1.6Hz,1H),2.29(dd,J=7.4,4.8Hz,2H),2.16(s,2H),2.05(d,J =6.6Hz,1H),2.03-1.99(m,1H),1.97-1.84(m,2H),1.81(d,J=9.6Hz,1H),1.61( q,J=6.0,3.8Hz,2H),1.07(t,J=7.2Hz,3H),1.00(s,9H),0.56(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ171.64,166.28,163.07,131.90,131.90,123.32,113.38,1 13.38,85.15,83.11,82.58,80.30,80.17,77.92,77.57,60.90,59.05,58.72,57 .66,56.07,55.83,55.38,53.96,50.70,48.94,48.85,48.28,48.06,44.91,42.15,39.00,37.44,36.14,34.95,30.84,29.55,29.55,29.55,26.34,15.31,13.52.

[0133] Example 90: Preparation of Compound 90 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of 3,3-dimethylbutyryl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was evaporated by rotation, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 59 NO 11 Pale yellow solid (71.1 mg), yield 61.9%. HRESIMS m / z:[(M+H) + ,742.40] 1 H NMR(400MHz,Chloroform-d)δ8.02(d,J=8.8Hz,2H),6.90(d,J=8.8Hz,2H),5.06(d,J=5.2Hz,1H),4.02(dd,J=8.8,5.6Hz,1H),3.95(d,J=6.8Hz,1H),3.85( d,J=0.8Hz,3H),3.61(d,J=8.4Hz,1H),3.40(dd,J=15.4,5.8Hz,1H),3.36(s, 3H),3.27(s,3H),3.22(s,3H),3.14(s,3H),3.02-2.98(m,2H),2.96(q,J=5.0 ,4.2Hz,2H),2.86-2.81(m,1H),2.59-2.52(m,1H),2.49(d,J=11.2Hz,1H),2. 45(q,J=2.4Hz,2H),2.43-2.39(m,1H),2.28(ddt,J=12.2,6.0,3.0Hz,1H),2. 17(s,2H),2.07(q,J=8.0,6.2Hz,2H),1.98-1.89(m,2H),1.79-1.71(m,1H),1 .60(dt,J=13.2,3.8Hz,2H),1.31(s,3H),1.08(t,J=7.0Hz,3H),1.00(s,9H). 13C NMR(100MHz,CDCl3)δ171.65,169.99,166.27,163.53,132.01,132.01,122.71,1 13.84,113.84,85.61,84.90,83.30,82.15,80.49,80.13,77.25,61.62,59.22,5 7.93, 57.93, 56.07, 55.56, 53.89, 50.35, 49.28, 49.13, 49.04, 48.32, 43.87, 41.89, 39.70, 39.19, 35.69, 35.05, 30.96, 29.64, 29.64, 29.64, 26.39, 21.82, 13.59.

[0134] Example 91: Preparation of Compound 91 100 mg of compound 2 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-bromobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 42 H 54 BrNO 10 Pale yellow solid (81.3 mg), yield 63.1%. HRESIMS m / z:[(M+H) + ,812.29] 1H NMR(400MHz,Chloroform-d)δ8.07(d,J=8.8Hz,2H),7.85(d,J=8.6Hz,2H),7.50(d,J=8.4Hz,2H),6.91(d,J=9.0Hz,2H),5.25(d,J=5.2Hz,1H),4.12(dd,J= 8.6,6.8Hz,1H),4.06-4.01(m,1H),3.85(s,3H),3.64(d,J=8.2Hz,1H),3.53- 3.44(m,1H),3.41-3.36(m,1H),3.30(s,6H),3.28(s,3H),3.24(s,3H),3.21(d d,J=8.2,6.8Hz,1H),3.09(d,J=8.2Hz,1H),3.03(dd,J=9.6,6.2Hz,1H),2.89 (s,1H),2.66(dt,J=6.4,3.2Hz,1H),2.53(dq,J=9.8,6.8,5.8Hz,2H),2.50-2. 44(m,2H),2.43-2.35(m,3H),2.35-2.31(m,1H),2.12-2.06(m,3H),1.91(dq, J=10.8,4.8Hz,1H),1.63(s,3H),1.11(t,J=7.2Hz,3H),0.65(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ166.46,165.15,163.34,132.11,132.11,131.62,131.62,131. 55,131.55,130.01,127.75,123.35,113.60,113.60,85.23,83.79,83.31,80.51,80 .31,78.16,77.36,61.07,59.19,58.88,58.14,56.25,56.07,55.53,54.09,50.90,49.11,49.01,48.28,45.28,42.31,39.18,37.64,36.23,35.09,26.48,15.50,13.66.

[0135] Example 92: Preparation of Compound 92 100 mg of breiaconitine A was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-bromobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 42 H 52 BrNO 11 Pale yellow solid (89.3 mg), yield 69.8%. HRESIMS m / z:[(M+H) + ,826.27] 1 H NMR(400MHz,Chloroform-d)δ8.06(d,J=8.8Hz,2H),7.84(d,J=8.6Hz,2H),7.50(d,J =8.6Hz,2H),6.92(d,J=8.8Hz,2H),5.27(d,J=5.2Hz,1H),4.12(dd,J=9.0,5.8Hz,1H) ,3.99(d,J=6.8Hz,1H),3.85(s,3H),3.63(d,J=8.4Hz,1H),3.58-3.52(m,1H),3.31(s ,3H),3.28(s,3H),3.25(s,3H),3.17(s,3H),3.11(d,J=23.2Hz,1H),3.05-3.01(m,3H ),2.90(td,J=5.8,5.4,1.8Hz,1H),2.63-2.57(m,1H),2.57-2.53(m,1H),2.51(t,J=5 .0Hz,1H),2.49-2.47(m,1H),2.45(t,J=3.4Hz,1H),2.30(ddd,J=12.6,6.2,3.4Hz,1H ),2.15-2.11(m,2H),2.11-2.04(m,1H),1.94(qd,J=7.4,6.6,3.2Hz,1H),1.76(dd,J= 8.8,4.0Hz,1H),1.62(qd,J=7.6,6.2,2.4Hz,2H),1.37(s,3H),1.11(t,J=7.2Hz,3H). 13 C NMR(100MHz,CDCl3)δ169.95,166.29,165.02,163.65,132.06,132.06,131.63,131. 63,131.49,131.49,129.80,127.84,122.61,113.91,113.91,85.59,84.83,83.37,8 3.15, 80.49, 80.26, 77.10, 61.67, 59.22, 58.30, 57.96, 56.11, 55.56, 53.88, 50.41, 49.34, 49.15, 49.08, 44.02, 41.90, 39.76, 39.22, 35.65, 35.06, 26.40, 21.85, 13.61.

[0136] Example 93: Preparation of Compound 93 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of thiophene acetyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 39 H 53 NO9S2, pale yellow solid (93.8 mg), yield 63.1%. HRESIMS m / z:[(M+H) + ,744.31] 1H NMR(400MHz,Chloroform-d)δ7.22(dd,J=5.2,1.2Hz,1H),7.19(dd,J=3.8,2.6Hz,1H),7.0 1(dt,J=3.2,1.2Hz,1H),6.97(dd,J=5.2,3.4Hz,1H),6.94(d,J=1.2Hz,1H),6.93(s,1H),4 .93(d,J=5.2Hz,1H),4.02-3.96(m,2H),3.92(t,J=7.8Hz,1H),3.83(s,2H),3.63(d,J=8.2 Hz,1H),3.51-3.46(m,1H),3.40-3.32(m,2H),3.30(s,6H),3.26(s,3H),3.18(s,3H),3.06( d,J=8.2Hz,1H),2.97(dd,J=9.4,6.2Hz,1H),2.77(s,1H),2.54-2.52(m,1H),2.50(q,J=3. 2,2.6Hz,1H),2.47(d,J=7.2Hz,1H),2.46-2.41(m,2H),2.38(d,J=1.6Hz,1H),2.24(dd,J=1 1.8,7.8Hz,2H),2.05(d,J=6.4Hz,1H),1.95(dd,J=7.2,4.8Hz,1H),1.87(dd,J=17.8,11.8 Hz,2H),1.73-1.68(m,1H),1.68-1.56(m,3H),1.10(t,J=6.8Hz,3H),1.06(t,J=7.2Hz,3H). 13 C NMR (100MHz, CDCl3) δ170.61,169.69,135.68,135.06,127.15,126.82,126.8 0,126.74,124.95,124.93,84.92,83.35,83.06,80.21,80.21,78.34,77.94,6 0.61,59.14,58.90,57.99,56.20,56.11,54.15,50.80,48.82,48.78,47.93,44.82,41.96,39.06,37.48,36.04,35.69,35.22,34.92,26.42,16.40,13.55.

[0137] Example 94: Preparation of Compound 94 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of p-trifluoromethoxybenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 43 H 51 F6NO 11 Pale yellow solid (119.0 mg), yield 68.3%. HRESIMS m / z:[(M+H) + ,872.33] 1 H NMR(400MHz,Chloroform-d)δ8.17(d,J=8.8Hz,2H),8.03(d,J=8.8Hz,2H),7.25(d ,J=8.8Hz,2H),7.19(d,J=7.4Hz,2H),5.27(d,J=5.2Hz,1H),4.15(t,J=7.4Hz,1H), 4.04-3.99(m,1H),3.65(d,J=8.2Hz,1H),3.51-3.46(m,1H),3.39(dd,J=8.2,6.8Hz ,1H),3.31(s,3H),3.29(s,3H),3.27(s,3H),3.24(s,3H),3.21-3.16(m,1H),3.07( d,J=8.2Hz,1H),3.05-3.00(m,1H),2.90(s,1H),2.70-2.65(m,1H),2.55(dd,J=4.4 ,2.8Hz,1H),2.52(dd,J=4.4,2.8Hz,1H),2.48(d,J=3.4Hz,1H),2.45(d,J=4.8Hz,1 H),2.40(s,1H),2.36(dd,J=7.6,3.6Hz,2H),2.34-2.28(m,1H),2.13-2.07(m,3H), 1.94-1.88(m,1H),1.69-1.59(m,2H),1.10(t,J=7.2Hz,3H),0.61(t,J=6.8Hz,3H). 13 C NMR(100MHz,CDCl3)δ165.42,164.61,152.64,152.55,132.05,132.05,132.05,131.89 ,131.89,131.89,129.40,129.26,120.29,120.29,120.29,120.29,85.25,83.81,83.2 2, 80.42, 80.25, 78.16, 77.99, 61.13, 59.12, 58.90, 58.18, 56.18, 56.09, 53.98, 50.87, 49.18, 49.02, 48.32, 45.27, 42.26, 39.18, 37.67, 36.20, 35.20, 26.45, 15.35, 13.64.

[0138] Example 95: Preparation of Compound 95 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of m-cyanobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the product was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 43 H 51 N3O9, pale yellow solid (111.0 mg), yield 73.7%. HRESIMS m / z:[(M+H) + ,754.36] 1H NMR(400MHz,Chloroform-d)δ8.43(t,J=1.6Hz,1H),8.35(dt,J=8.0,1.4Hz,1H),8.27(t,J =1.6Hz,1H),8.21(dt,J=8.0,1.4Hz,1H),7.80(ddt,J=16.2,7.8,1.4Hz,2H),7.58(t,J=7. 8Hz,1H),7.52(t,J=7.8Hz,1H),5.30(d,J=5.2Hz,1H),4.17(dd,J=8.8,5.8Hz,1H),4.00(d d,J=6.6,1.4Hz,1H),3.66(d,J=8.2Hz,1H),3.52-3.45(m,1H),3.41(dd,J=8.4,6.8Hz,1H) ,3.30(s,3H),3.29(s,3H),3.27(s,3H),3.23(s,3H),3.22-3.16(m,1H),3.07-3.00(m,2H) ,2.90(s,1H),2.68(dt,J=7.0,3.4Hz,1H),2.59-2.53(m,1H),2.53-2.48(m,2H),2.46(dt, J=7.2,3.4Hz,1H),2.44-2.38(m,2H),2.38-2.35(m,1H),2.33(d,J=5.7Hz,1H),2.15-2.08 (m,3H),1.97-1.88(m,1H),1.72-1.56(m,2H),1.10(t,J=7.2Hz,3H),0.64(t,J=6.8Hz,3H). 13 C NMR (100MHz, CDCl3) δ164.53,163.73,135.96,135.87,134.12,133.97,133.92,133.65 ,132.09,132.04,129.47,129.40,118.20,118.11,112.87,112.85,85.26,84.37,83.0 9,80.15,80.03,78.13,78.13,61.35,59.13,58.96,58.08,56.18,56.18,53.78,50.82,49.22,49.11,48.32,45.31,42.15,39.16,37.57,36.06,35.29,26.40,15.53,13.65.

[0139] Example 96: Preparation of Compound 96 100 mg of compound 4 was weighed and placed in a 5 mL round-bottom flask. 2 ml of dried pyridine was added to dissolve it, and under Ar gas protection, two equivalents of 3,5-dinitrobenzoyl chloride were added in an ice bath. The reaction was carried out at room temperature (approximately 20°C), and the progress of the reaction was detected by thin-layer chromatography. After approximately 12 hours, the target product was formed along with the by-products. The reaction mixture was rotated and evaporated, and the compound was separated and purified by column chromatography to obtain the target compound. Its structure and characteristics are as follows. [ka] Molecular formula C 41 H 49 N5O 17 Pale yellow solid (114.1 mg), yield 64.6%. HRESIMS m / z:[(M+H) + ,884.31] 1 H NMR(400MHz,Chloroform-d)δ9.32(d,J=2.2Hz,2H),9.22(t,J=2.2Hz,1H),9.17(t,J=2.2Hz,1H),9.09(d,J=2.2Hz,2H),5.44(d,J=5.2Hz,1H),4.2 5(dd,J=9.0,4.8Hz,1H),4.02(d,J=6.6Hz,1H),3.69(d,J=8.2Hz,1H),3.4 9-3.41(m,2H),3.34(s,3H),3.31(s,3H),3.30(s,3H),3.26(s,3H),3.10- 3.03(m,2H),2.95(s,1H),2.76(dt,J=5.8,3.2Hz,1H),2.62-2.56(m,1H), 2.54(dd,J=6.4,4.6Hz,2H),2.51-2.43(m,3H),2.40(dd,J=15.2,5.0Hz,2 H),2.19(dd,J=8.0,5.0Hz,3H),1.71(dq,J=13.8,6.8,4.6Hz,2H),1.61(d dd,J=15.6,6.2,2.8Hz,2H),1.12(t,J=7.2Hz,3H),0.65(t,J=6.8Hz,3H). 13C NMR(100MHz,CDCl3)δ162.28,161.55,148.66,148.66,148.60,148.60,134.37,13 4.37,129.94,129.94,129.68,129.68,122.30,122.25,85.87,85.29,82.89,79.99 ,79.34,78.51,78.04,61.64,59.05,59.00,57.78,56.25,56.08,53.48,50.76,49.36,49.16,48.40,45.38,42.15,39.15,37.12,35.58,35.43,22.67,15.68,13.61.

[0140] The beneficial effects of the present invention will be demonstrated below through experimental examples.

[0141] Experimental Example 1: Anti-inflammatory and analgesic activity and toxicity test of the compound of the present invention 1. Laboratory animals and samples Test animals: Kunming mice (half male and half female; weight 22±2g) provided by Chengdu Dashuo Laboratory Animals Co., Ltd. The mice were housed in the animal room of the Laboratory Animal Research Institute of Sichuan Provincial Academy of Medical Sciences and Sichuan Provincial Citizens' Hospital, where the temperature was maintained at 23±2℃, the humidity at 55±5%, and the photoperiod at 16:8h (L:D). Before the experiment, the mice were adaptively reared for 2-3 days with free access to water and food. For 12 hours prior to the experiment, the mice were fasted but not deprived of water. Each group consisted of 10 test animals, and at least 6 usable data points were secured for each group. The animal experiments were conducted strictly in accordance with relevant regulations on laboratory animal management in China.

[0142] Test samples: The compounds obtained in the examples of the present invention (tested sample group) and breiaconitine A (positive control group) were each dissolved in 0.1 mol / L hydrochloric acid in a 1:1 molar ratio, and then diluted with physiological saline to the planned concentration for measurement. The blank control was physiological saline containing 0.1 mol / L hydrochloric acid. Except for changing the tested sample to physiological saline, the control group animals underwent the same treatment as the experimental group.

[0143] 2. Experimental Method (1) Measurement of analgesic activity (acetic acid rising method): Ten mice were randomly selected (half male and half female) and placed in separate mouse cages. The sample solution to be measured was injected subcutaneously into each mouse at a dose of 0.1 mL / 10 g body weight. After 15 minutes, a 0.7% acetic acid solution was injected intraperitoneally, and the mice were observed and the number of rising responses in each mouse within 15 minutes was recorded. The blank group was subcutaneously injected with physiological saline, the experimental group was injected with the sample to be measured, and the positive group was injected with breiaconitine A. Analgesic activity is expressed as the percentage reduction in the number of risings compared to the blank group (rising inhibition rate). The specific calculation formula is as follows. Rising suppression rate (pain relief rate) = (Average number of risings in the blank group - Average number of risings in the experimental group) / Average number of risings in the blank group × 100%

[0144] 50% effective dose (ED) 50 Measurement: The drug to be measured was dissolved in a 0.1 mol / L HCl solution in a 1:1 molar ratio, and then diluted geometrically with physiological saline to create at least five different dose-concentration groups. The rising inhibition rate for each dose group was measured using the above method, which measures analgesic activity by acetic acid rising. The obtained dose-inhibition rate data were entered into SPSS software (version 17.2), and the ED of the samples was determined by probit regression. 50 I calculated it.

[0145] (2) Acute toxicity and median lethal dose (LD50) 50 Measurement of LD50 (LD50) was performed by dissolving the drug in a 1:1 molar ratio in a 0.1 mol / L HCl solution, diluting it to the desired concentration with physiological saline, randomly selecting 10 mice from each group (half male and half female), placing them in separate cages, and subcutaneously injecting them with different sample solutions at a dose of 0.1 mL / 10 g body weight. In the acute toxicity preliminary experiment, the measurement concentration was set to 20 mg / kg, and then, based on the survival rate of the experimental animals obtained in the preliminary experiment, the drug was divided into at least 5 concentration / dose groups in a geometric progression. The survival rate of the mice within 24 hours was recorded by observation. The obtained dose-survival rate data was entered into SPSS software (version 17.2), and the LD50 of the drug was determined by probit regression. 50 I calculated it.

[0146] (3) Calculation of the Therapeutic Index (TI) value: The therapeutic index of the compound was calculated based on the 50% effective dose and the median lethal dose. The specific calculation formula is as follows. Therapeutic Index (TI) = Median Lethal Dose (LD50) / 50% Effective Dose (ED) 50 ).

[0147] (4) Measurement of anti-inflammatory activity: The effect of the compound at a concentration of 30 μM on the cellular activity of RAW264.7 cells was measured using the MTT method. The suppression of NO release in the LPS-induced inflammatory response of RAW264.7 cells by the compound at a concentration of 30 μM was measured using the Griess method. The specific methods are as follows.

[0148] MTT method: MTT was prepared in a 5 mg / ml solution using PBS buffer, filtered and sterilized using a 0.22 μm filter membrane, and then stored in a dark place under refrigeration. Each compound was accurately weighed, a 50 mmol / L mother liquor was prepared with DMSO, frozen and stored in a dark place, and then diluted to a 30 μmol / L solution with DMEM containing 10% FBS. RAW264.7 cells of three or more generations were added to the culture medium, and a cell suspension was prepared by gently pipetting until the cells detached. 10 μL was aspirated and placed on a glass slide, and after counting, 6 × 10⁶ 3 Cells were inoculated into a 96-well plate at 1 / well, with 100 μL of cell suspension in each well. After incubation at 37°C and 5% CO2 for 24 hours, the supernatant was aspirated. 100 μL of medium was added to each well of the zero group (CO group), and 100 μL of LDMSO (1 / 1000) was added to each well of the blank group (CK group). The sample to be measured (100 μL / well) was added to the experimental group. After 12 hours, the supernatant was aspirated, 5 μg / ml of MTT (120 μL / well) was added, and the cells were incubated at CO2 for 4 hours. After incubation, the supernatant was aspirated, DMSO (150 μL / well) was added, and the mixture was shaken for 10 minutes (50 r / min) in a shaker. The absorbance was measured at 492 nm. The relative cell activity (%) was calculated using the following formula. Cell-relative activity (%) = (OD 実験 -OD CO ) / (OD CK -OD CO) × 100%.

[0149] Griess method: Add RAW264.7 cells of 3 generations or more to the culture medium, gently pipette until the cells detach, prepare a cell suspension, aspirate 10 μL and place it on a glass slide, count the cells, and then measure 3 × 10 4 Cells were inoculated into 96-well plates, with 100 μL of cell suspension in each well. After incubation at 37°C and 5% CO2 for 24 hours, the supernatant was aspirated. 100 μL of DMSO (1 / 1000) was added to each well of the blank and LPS groups. The test sample (100 μL / well) was added to the experimental group. After 2 hours, 1 μg / ml of LPS (3 μL / well) was added to both the LPS and experimental groups. After 22 hours, 50 μL of supernatant was aspirated and placed in a new 96-well plate. Griess Reagent I (50 μL / well) from the NO kit was added, followed by Griess Reagent II (50 μL / well). Absorbance values ​​were read at 562 nm and substituted into the standard curve to calculate the NO content. Calculation formula: NO inhibition rate (%) = (OD LPS -OD 実験 ) / (OD LPS -OD ブランク ).

[0150] 3. Experimental Results Table 1: Analgesic activity and acute toxicity of each compound [Table 1] TIFF2026511621000118.tif254170TIFF2026511621000119.tif118170 a The mice showed clear signs of poisoning or death, and no analgesia rate was observed. In the blank group, physiological saline containing 0.1 mol / L HCl was used. b A 0% analgesic rate indicates that, under current experimental conditions, the inhibitory effect of this drug is below the detection limit or does not show a significant difference compared to other treatment groups. cIn acute toxicity experiments, mice were administered at a concentration of 20 mg / kg, and their deaths were observed within 24 hours. If death occurred, it was recorded as positive (+); if not, it was recorded as negative (-). *P<0.05; **P<0.01.

[0151] Table 2: ED of some compounds 50 LD 50 and treatment index [Table 2] a LD in the table 50 >X, when animals are treated with a drug concentration of X mg / kg under current experimental conditions, does not result in death or toxicity, and LD 50 This indicates that the concentration may be higher than this. 50 This needs to be confirmed through further experiments.

[0152] Table 3: Compound suppression rates of NO production in LPS-induced RAW264.7 cells [Table 3]

[0153] First, the effective dose of 50% of breiaconitine A as described in the literature (ED 50 The analgesic activity of the compounds was evaluated using an initial screening concentration of 0.05 mg / kg, and the acute toxicity of the compounds was evaluated by subcutaneous injection (initial concentration 20 mg / kg) (Table 1). As can be seen from the data in Table 1, all compounds obtained in the examples of the present invention, except for compounds 1 and 2, did not cause death in mice in the initial acute toxicity evaluation experiment, and their toxicity was far lower than that of breiaconitine A. Most of the compounds showed analgesic activity equivalent to breiaconitine A (based on an analgesic rate of 49% or higher). Therefore, compounds with an analgesic rate of 49% or higher were selected for 50% effective dose ED. 50The following was measured. Furthermore, since the compounds obtained in the examples of the present invention have low acute toxicity, the remaining compounds with relatively high analgesic activity (based on an analgesic rate of 40% or more in the initial screening activity) were selected and administered at 0.5 mg / kg (Table 1), and compounds with an analgesic rate of 60% or more at this concentration were selected for a 50% effective dose ED. 50 The median lethal dose (LD50) of the preferred compounds listed above was measured. 50 The following was measured. As can be seen from the data in Table 2, all of the preferred compounds listed above showed activity equivalent to that of breiaconitine A, but their toxicity was far lower than that of breiaconitine A, and their corresponding therapeutic indices were all higher than those of breiaconitine A.

[0154] Furthermore, the anti-inflammatory activity of the compounds was evaluated, and RAW cytotoxicity experiments were performed on compounds that had lower toxicity than breiaconitine A and good analgesic activity (based on an analgesic rate of 40% or more in initial screening activity) (Table 3). Subsequently, NO inhibition experiments were performed on compounds with a RAW cell viability of 85% or more to investigate their anti-inflammatory activity. As can be seen from the data in Table 3, some compounds have good anti-inflammatory activity (based on an NO inhibition rate of 40% or more) (Table 3).

[0155] As can be seen from the experimental results above, the compounds obtained in this invention have good analgesic and anti-inflammatory activity and low toxicity, and can be used in the preparation of effective and low-toxicity analgesics.

Claims

1. A compound represented by the following formula I, its isomer, its deuterated compound, its solvate, its prodrug, its metabolite, its crystalline form, or its pharmaceutically acceptable salt. 【Chemistry 1】 Equation I (R １ , R ２ , R ３ , R ４ , R ５ are each independently hydrogen, hydroxyl, halogen, C １～１８ alkoxy, C １～１８ alkyl, COOR ａ , OCOR ａ selected from, R ａ is hydrogen, C １～１８ alkyl, phenyl, 3-6 member heteroaryl, 3-8 member saturated cycloalkyl, 3-8 member saturated heterocyclyl, fused cycloalkyl, hetero fused ring group, bicycloalkyl, heterobicyclyl selected from, R ６ , R ７ These are, independently, hydrogen, hydroxyl, and C. １～１８ Alkoxy, C １～１８ Alkyl, OCOR ｂ , OCOCH ２ R ｂ OSO ２ R ｂ Selected from, R ｂ is hydrogen, one or more R ｚ C replaced by １～６ Alkyl, one or more R ｚ C replaced by ２～６ Alkenyl, one or more R ｚ C replaced by ２～６ Alkinyl, one or more R ｚ Phenyl substituted with, one or more R ｚ A 3- to 6-membered heteroaryl substituted with one or more R ｚ A 3- to 8-membered saturated cycloalkyl group substituted with one or more R ｚ A 3- to 8-membered saturated heterocycline substituted with one or more R ｚ A condensed cycloalkyl group substituted with one or more R ｚ A heterocondensed ring group substituted with, one or more R ｚ Bicycloalkyl substituted with, one or more R ｚ Selected from heterobisicrills substituted with, The aforementioned R ｚ These are, independently, hydrogen, substituted or unsubstituted C １～６ Alkyl, C ２～６ Alkenil, C ２～６ Alkynyl, substituted or unsubstituted C １～６ Alkoxy, 3-8 member saturated cycloalkyl, NR ３ R ４ COOR ５ SO ２ R ６ Selected from halogen, cyano, nitro, hydroxyl, carboxyl, and phenyl, the C １～６ Alkyl, C １～６ The alkoxy replacement group is selected from halogen, cyano, nitro, hydroxyl, and carboxyl groups.

2. The compound according to claim 1, its isomer, its deuterated compound, its solvate, its prodrug, its metabolite, its crystalline form, or its pharmaceutically acceptable salt, characterized in that the structure of the compound is represented by the following formula II. 【Chemistry 2】 Formula II (In the formula, R ５ is hydrogen, hydroxyl, halogen, C １～１８ Alkoxy, C １～１８ Alkyl, COOR ａ ,OCOR ａ Selected from, R ａ is hydrogen, C １～１８ Selected from alkyl, phenyl, 3-6 membered heteroaryl, 3-8 membered saturated cycloalkyl, 3-8 membered saturated heterocyclyl, condensed cycloalkyl, heterocondensed ring group, bicycloalkyl, and heterobicyclyl. R ６ , R ７ These are, independently, hydrogen, hydroxyl, and C. １～１８ Alkoxy, C １～１８ Alkyl, OCOR ｂ , OCOCH ２ R ｂ OSO ２ R ｂ Selected from, R ｂ is hydrogen, one or more R ｚ C replaced by １～６ Alkyl, one or more R ｚ C replaced by ２～６ Alkenyl, one or more R ｚ C replaced by ２～６ Alkinyl, one or more R ｚ Phenyl substituted with, one or more R ｚ A 3- to 6-membered heteroaryl substituted with one or more R ｚ A 3- to 8-membered saturated cycloalkyl group substituted with one or more R ｚ A 3- to 8-membered saturated heterocycline substituted with one or more R ｚ A condensed cycloalkyl group substituted with one or more R ｚ A heterocondensed ring group substituted with, one or more R ｚ Bicycloalkyl substituted with, one or more R ｚ Selected from heterobisicrills substituted with, Said R ｚ each independently represents hydrogen, substituted or unsubstituted C １～６ alkyl, C ２～６ alkenyl, C ２～６ alkynyl, substituted or unsubstituted C １～６ alkoxy, a 3- to 8-membered saturated cycloalkyl, NR ３ R ４ , COOR ５ , SO ２ R ６ , halogen, cyano, nitro, hydroxyl, carboxyl, phenyl, and the substituents of said C １～６ alkyl and C １～６ alkoxy are selected from halogen, cyano, nitro, hydroxyl, carboxyl, and R ３ , R ４ each independently represents hydrogen or C １～６ alkyl. )

3. The compound according to claim 2, its isomer, its deuterated compound, its solvate, its prodrug, its metabolite, its crystalline form, or its pharmaceutically acceptable salt, characterized in that the structure of the compound is represented by the following formula III. 【Transformation 3】 Formula III (wherein, R ６ , R ７ are each independently hydrogen, hydroxyl, C １～６ alkoxy, C １～６ alkyl, OCOR ｂ , OCOCH ２ R ｂ , OSO ２ R ｂ and are selected from R ｂ is hydrogen, one or more R ｚ C replaced by １～６ Alkyl, one or more R ｚ C replaced by ２～６ Alkenyl, one or more R ｚ C replaced by ２～６ Alkinyl, one or more R ｚ Phenyl substituted with, one or more R ｚ A 3- to 6-membered heteroaryl substituted with one or more R ｚ A 3- to 8-membered saturated cycloalkyl group substituted with one or more R ｚ A 3- to 8-membered saturated heterocycline substituted with one or more R ｚ A condensed cycloalkyl group substituted with one or more R ｚ A heterocondensed ring group substituted with, one or more R ｚ Bicycloalkyl substituted with, one or more R ｚ Selected from heterobisicrills substituted with, The aforementioned R ｚ These are, independently, hydrogen, halogenated or non-halogenated C. １～６ Alkyl, C ２～６ Alkenil, C ２～６ Alkynyl, halogenated, or non-halogenated C １～６ Alkoxy, 3-8 member saturated cycloalkyl, NR ３ R ４ COOR ５ SO ２ R ６ Selected from halogen, cyano, nitro, hydroxyl, carboxyl, and phenyl, R ３ , R ４ These are hydrogen and C, respectively, independently. １～６ Selected from alkyl groups, R ５ C １～６ Selected from alkyl groups.

4. The compound according to claim 2, its isomer, its deuterated compound, its solvate, its prodrug, its metabolite, its crystalline form, or its pharmaceutically acceptable salt, characterized in that the structure of the compound is represented by the following formula IV. 【Chemistry 4】 Formula IV (In the formula, R ６ , R ７ These are, independently, hydrogen, hydroxyl, and C. １～６ Alkoxy, C １～６ Alkyl, OCOR ｂ , OCOCH ２ R ｂ OSO ２ R ｂ Selected from, R ｂ is hydrogen, one or more R ｚ C replaced by １～６ Alkyl, one or more R ｚ C replaced by ２～６ Alkenyl, one or more R ｚ C replaced by ２～６ Alkinyl, one or more R ｚ Phenyl substituted with, one or more R ｚ A 3- to 6-membered heteroaryl substituted with one or more R ｚ A 3- to 8-membered saturated cycloalkyl group substituted with one or more R ｚ A 3- to 8-membered saturated heterocycline substituted with one or more R ｚ A condensed cycloalkyl group substituted with one or more R ｚ A heterocondensed ring group substituted with, one or more R ｚ Bicycloalkyl substituted with, one or more R ｚ Selected from heterobisicrills substituted with, The aforementioned R ｚ These are, independently, hydrogen, halogenated or non-halogenated C. １～６ Alkyl, C ２～６ Alkenil, C ２～６ Alkynyl, halogenated, or non-halogenated C １～６ Alkoxy, 3-8 member saturated cycloalkyl, NR ３ R ４ COOR ５ SO ２ R ６ Selected from halogen, cyano, nitro, hydroxyl, carboxyl, and phenyl, R ３ , R ４ These are hydrogen and C, respectively, independently. １～６ Selected from alkyl groups, R ５ C １～６ Selected from alkyl groups.

5. The compound according to claim 2, its isomer, its deuterated compound, its solvate, its prodrug, its metabolite, its crystalline form, or its pharmaceutically acceptable salt, characterized in that the structure of the compound is represented by the following formula V. 【Transformation 5】 Formula V (In the formula, R ６ , R ７ These are, independently, hydrogen, hydroxyl, and C. １～６ Alkoxy, C １～６ Alkyl, OCOR ｂ , OCOCH ２ R ｂ OSO ２ R ｂ Selected from, R ｂ is hydrogen, one or more R ｚ C replaced by １～６ Alkyl, one or more R ｚ C replaced by ２～６ Alkenyl, one or more R ｚ C replaced by ２～６ Alkinyl, one or more R ｚ Phenyl substituted with, one or more R ｚ A 3- to 6-membered heteroaryl substituted with one or more R ｚ A 3- to 8-membered saturated cycloalkyl group substituted with one or more R ｚ A 3- to 8-membered saturated heterocycline substituted with one or more R ｚ A condensed cycloalkyl group substituted with one or more R ｚ A heterocondensed ring group substituted with, one or more R ｚ Bicycloalkyl substituted with, one or more R ｚ Selected from heterobisicrills substituted with, The aforementioned R ｚ These are, independently, hydrogen, halogenated or non-halogenated C. １～６ Alkyl, C ２～６ Alkenil, C ２～６ Alkynyl, halogenated, or non-halogenated C １～６ Alkoxy, 3-8 member saturated cycloalkyl, NR ３ R ４ COOR ５ SO ２ R ６ Selected from halogen, cyano, nitro, hydroxyl, carboxyl, and phenyl, R ３ , R ４ These are hydrogen and C, respectively, independently. １～６ Selected from alkyl groups, R ５ C １～６ Selected from alkyl groups.

6. The structure of the compound is selected from the following structures, and the compound, isomer thereof, deuterated compound thereof, solvate thereof, prodrug thereof, metabolite thereof, crystalline form thereof, or pharmaceutically acceptable salt thereof according to any one of claims 1 to 5. 【Transformation 6】 【change】 【change】 【change】 【change】 【change】 【change】

7. A pharmaceutical composition for analgesia and / or anti-inflammatory purposes, characterized by comprising as an active ingredient a compound according to any one of claims 1 to 6, an isomer thereof, a deuterated compound thereof, a solvate thereof, a prodrug thereof, a metabolite thereof, a crystalline form thereof, or a pharmaceutically acceptable salt thereof, and further comprising a pharmaceutically acceptable adjuvant.

8. Use in the preparation of any one of the compounds, isomers thereof, deuterated compounds thereof, solvates thereof, prodrugs thereof, metabolites thereof, crystalline forms thereof, or pharmaceutically acceptable salts thereof, in the preparation of analgesic and / or anti-inflammatory agents.

9. The use according to claim 8, characterized in that the analgesic and / or anti-inflammatory agent is a low-toxicity analgesic and / or anti-inflammatory agent.

10. The use according to claim 9, characterized in that the median lethal dose of the analgesic and / or anti-inflammatory drug is higher than the median lethal dose of breiaconitine A, and / or the therapeutic index of the analgesic and / or anti-inflammatory drug is higher than the therapeutic index of breiaconitine A.

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