69 results about "Propargyl" patented technology

The invention belongs to the field of medicinal chemistry, and relates to an indole allylamine amide derivative as well as a preparation method and application thereof. Functional activity screening of G protein dependent signaling pathways is carried out on all the synthesized compounds, and it is found that the new derivatives can be used for preparing beta2-adrenergic receptor allosteric antagonism regulator drugs. Trans-indole allylamine is used as a raw material, amide coupling is performed to obtain the novel indole allylamine amide derivative, and R1 is any one of phenyl, m-methylbenzene, m-methoxyphenyl, m-bromophenyl, m-chlorphenyl, m-fluorophenyl, o-methoxyphenyl, p-methoxyphenyl, naphthalene ring, oxazole, cyclohexyl, cyclopentyl, methyl, ethyl and isopropyl. A biological activity test result shows that the indole allylamine amide derivative disclosed by the invention has relatively good antagonistic activity on beta2AR and can be used for carrying out negative allosteric regulation on the functional activity of isoproterenol.

The invention provides an application of combination of SPRC and a PD-1 or PD-L1 inhibitor in preparation of a lung cancer immunotherapy sensitizing drug, and relates to the technical field of biomedicine.In the application, through in-vitro cell experiments, cell co-culture experiments and in-vivo animal experiments, S-propargyl-L-cysteine (SPRC) can play a sensitizing role in the anti-lung cancer curative effect of the PD-1 inhibitor, and can be used for preparing a sensitizing drug for lung cancer immunotherapy. The core mechanism is as follows: 30 [mu] M SPRC is in a non-cytotoxic dose window and can specifically inhibit IFN-gamma induced STAT1 phosphorylation and PD-L1 up-regulation by depending on a CSE / H2S pathway, while IFN-gamma-STAT1-PD-L1 is a core signal axis of PD-L1 adaptive up-regulation in lung cancer cells, and the induction effect of TNF-alpha on PD-L1 is relatively weak; meanwhile, SPRC can inhibit activation of NF-kB induced by TNF-alpha and expression of inflammatory factors such as IL-6 and IL-8 through the pathway so as to exert the anti-inflammatory effect, the CD8 + T cell depletion proportion can be remarkably reduced by combining SPRC with anti-PD-1, the synergistic tumor inhibition effect is formed, the effect is verified in in-vivo and in-vitro experiments, and a closed loop of an in-vitro mechanism and an in-vivo curative effect is achieved.

The invention relates to a method for synthesizing an iodo-pyridine compound from N-propargyl enaminone, which comprises the following steps: by taking N-propargyl enaminone as a raw material, DMF (Dimethyl Formamide) as a reaction solvent and copper acetate and N-iodosuccinimide as accelerators, carrying out intramolecular coupling reaction at 60 DEG C to synthesize the iodo-pyridine compound. The method for directly synthesizing the pyridine heterocyclic compound through the intramolecular coupling reaction of the N-propargyl enaminone under the non-alkaline condition is disclosed for the first time, reaction substrates are not limited to benzene rings on alkynyl, the application range of the reaction is greatly expanded, and the method has the advantages of being wide in substrate range, strong in functional group application range, mild in reaction condition, easy to operate, safe, high in yield and the like. And raw materials are cheap.

The application belongs to the technical field of nanofiltration, and provides a preparation method of recrystallized silicon carbide-silicon carbon nitride ceramic membrane. The application obtains a pyrolytic material by first applying a polysilazane solution on a porous base and then performing first pyrolysis; and obtains the recrystallized silicon carbide-silicon carbon nitride ceramic membrane by second applying the polysilazane solution on the pyrolytic material and then performing second pyrolysis. The application uses a solution containing propargyl polysilazane or an organic polysilazane Durazane 1500 rapid cure fast-drying resin as a precursor to prepare the ceramic membrane, and the ceramic membrane has high ceramic yield, excellent high-temperature stability, high rejection rate and controllable microstructure, and is suitable for separation and protection applications in extreme environments.

The application discloses a propargyl polysiloxane modified cyanate ester resin and a preparation method and application thereof, and comprises the following steps: S1, a propargyl compound shown in formula I and polysiloxane shown in formula II are subjected to a heating reaction in the presence of a platinum catalyst and a solvent to obtain a propargyl polysiloxane; S2, the propargyl polysiloxane is mixed with a cyanate ester monomer, heated and stirred until a transparent solution is obtained, and subjected to a heat curing treatment to obtain the propargyl polysiloxane modified cyanate ester resin. The propargyl polysiloxane modified cyanate ester resin can be cured and formed at a lower curing temperature, and the prepared modified resin has lower dielectric loss, water absorption, higher impact strength and thermal stability, and has a good application prospect in high-end electronic materials.

This invention relates to a novel use of propargylcysteine ​​in the preparation of anti-mastopathy drugs. The invention discovers that S-propargylcysteine ​​can improve E2 / P imbalance by regulating HPO axis function and inhibiting abnormal activation of the GnRH-sex hormone axis; it also reduces the inflammatory microenvironment by inhibiting the release of inflammatory factors; ultimately, it downregulates ER / PR-mediated proliferation signals and inhibits PCNA expression locally in the breast. Through multi-target regulation of neuroendocrine, inflammatory responses, and proliferation-related signaling pathways, it effectively alleviates breast hyperplasia and its associated chronic stress-induced depressive-like behaviors, thus exerting anti-mastopathy and therapeutic effects on breast hyperplasia complicated with depression.

This disclosure relates to a process for the synthesis of a compound of formula (I): (I) wherein w, x, y, and z are as defined in the description. The process includes the reaction of a compound of formula (II): (II) with carbonyldiimidazole, and the reaction of the resulting compound with propargylamine.

The present disclosure relates, in one aspect, to propargyl amino-ionizable lipid compounds of formula (I), and methods of preparing the same. In another aspect, the disclosure relates to lipid nanoparticles (LNPs) comprising at least one ionizable lipid of formula (I) or (III). In another aspect, the LNPs of the disclosure are useful for gene editing applications. In another aspect, the LNPs of the disclosure are useful for splenic delivery of therapeutic cargo.

The invention relates to a nano nickel electroplating process used after secondary zinc deposition of an aluminum alloy. The nano nickel electroplating process comprises two steps of preparing a plating solution and electroplating. A nano nickel agent A and a nano nickel agent B are added into the plating solution, and the nano nickel agent A comprises, by mass, 5%-9% of nickel sulfate, 6%-10% of sodium propargyl sulfonate, 5%-9% of sodium hypophosphite monohydrate and 72%-84% of deionized water; and the nano nickel B agent comprises the following components in percentage by mass: 5-9% of butynol alcohol ether sodium propane sulfonate, 6-10% of sodium propargyl sulfonate, 5-9% of sodium hypophosphite monohydrate and 72-84% of deionized water. Sodium propargyl sulfonate is coordinated with Ni < 2 + > in a high-activity area of a workpiece through electrostatic adsorption and coordination so as to inhibit deposition of Ni < 2 + >; the surface energy of a low-activity area of the workpiece is low, Ni < 2 + > deposition is basically not affected, negatively-charged propargyl sulfonate radicals can be attracted by weak positive charges in the area, and continuous generation of new crystal nucleuses is promoted. The sodium hypophosphite monohydrate can prevent Ni < 2 + > from being oxidized through reaction with oxygen. Butynol alcohol ether sodium propane sulfonate inhibits overgrowth of crystal grains and refines the crystal grain structure through adsorption and steric hindrance effect.

The application relates to the technical field of acoustic materials, in particular to a sound matching material, a preparation method thereof, an ultrasonic transducer, an ultrasonic probe and an ultrasonic imaging device. The sound matching material comprises a polystyrene telechelic polymer with a chemical structure as shown in formula I: wherein n1 and n2 are positive integers; X comprises at least one of halogen atoms, hydroxyl groups, carboxyl groups, amino groups, propargyl groups, methoxyl groups, azido groups, pyrimidyl groups and malonate groups. The sound matching material has not only good low sound attenuation characteristics, but also good bonding performance, can improve the stable reliability of sound transmission, and has a good application prospect in medical ultrasonic probes.

The invention relates to the technical field of detection, in particular to a method for determining the content of propargyl and / or isopropargyl by using nuclear magnetic resonance. The method comprises the following steps: preparing a detection solution by taking dimethyl terephthalate as an internal standard substance and propargyl or isopropargyl as a detection sample, then carrying out nuclear magnetic resonance measurement, respectively establishing linear regression equations, and determining that the isopropargyl is Y1 = 0.2214 X1-0.0236 and R12 = 0.99082; the Y2 is equal to 0.6524, the X < 2 > is equal to 0.0104, and the R22 is equal to 0.99981. Then performing NMR measurement on a to-be-measured solution to obtain a quantitative peak area, and substituting the quantitative peak area into the equation to obtain the content. According to the method, a standard substance is not needed, a specific quantitative peak is selected to avoid interference, the detection linear range is 0.05 mg / mL-20 mg / mL, the detection limit is 0.02 mg / mL, operation is easy and convenient, cost is low, accuracy and reliability are achieved, and the method is suitable for content detection of propargyl and / or isopropargyl.

This invention discloses a method for synthesizing chiral quinoxalones. Using a copper salt, a chiral ligand, and a base as a catalytic system, the target chiral quinoxalone compound is obtained by reaction in an organic solvent. This invention utilizes an economical and readily available copper catalyst, constructing C-N bonds through propargyl substitution and aminolysis of the ester group to synthesize chiral quinoxalones. This method has advantages such as good substrate universality, high yield, good enantioselectivity, and ease of industrial production. The synthesis method of this invention does not require the use of special and expensive catalysts, and the reaction conditions are simple, requiring no special reaction environment such as high-pressure hydrogen, with low requirements for reaction equipment, making it easy to scale up for industrial production.

The application discloses a self-curable propargyl polysiloxane monomer and a preparation method and application thereof, the propargyl polysiloxane is obtained by reacting a propargyl compound shown in formula I with a polysiloxane shown in formula II, is liquid at room temperature, and can be self-cured to form a resin at high temperature. The resin formed by self-curing the propargyl polysiloxane as a monomer has an initial thermal decomposition temperature of up to 503.3 DEG C under a nitrogen atmosphere, a carbon residue rate of up to 83.1% at 800 DEG C, and a total heat release amount of only 4.8 kJ˙g ‑1 , a heat release capacity of only 33.6 J˙g ‑1 , ‑1 , and a peak temperature of 518.8 DEG C, and exhibits outstanding thermal stability and flame retardancy, can effectively inhibit the chemical combustion reaction of a flame, and has a good application prospect in the fields of aerospace, insulating electricity, building materials and the like.

The invention discloses a carbon dot corrosion inhibitor with excellent corrosion inhibition and tracing performance, a preparation method and application, and relates to the technical field of corrosion inhibition of metal materials. The technical problems that in the prior art, a carbon dot corrosion inhibitor is prone to aggregation and instability in a high-temperature and strong-acid environment, and application is single are solved. The method comprises the following steps: firstly, taking citric acid and propargyl-PEG2-amine as raw materials, and dissolving the raw materials in deionized water to obtain a mixed solution; the mixed solution is placed in a high-pressure reaction kettle to be subjected to a hydrothermal reaction, and citric acid carbon dots modified by propargyl-PEG2-amine are prepared; sequentially carrying out centrifugation, dialysis and freeze drying treatment on the citric acid carbon dots modified by the propargyl-PEG2-amine, so as to obtain the citric acid carbon dots modified by the propargyl-PEG2-amine. The prepared carbon dot corrosion inhibitor can be used as a corrosion inhibition material in a high-temperature-resistant strong-acid environment, and can also be used for in-situ monitoring of dichromate ions in industrial wastewater and in-situ monitoring of iron ions and ferrous ions in underground water, surface water and drinking water so as to judge whether the content of the iron ions and the ferrous ions exceeds the standard or not.

The invention relates to the technical field of fluorescence detection and molecular probes, in particular to a fluorescent probe for detecting bivalent palladium as well as a preparation method and application of the fluorescent probe. The fluorescent probe for detecting bivalent palladium is a compound with a structure shown in a formula (I). The fluorescent probe provided by the invention takes benzopyran as a fluorescent parent nucleus and propynyl as a recognition site, and is novel in structure. When the fluorescent probe is used for divalent palladium detection, the fluorescent probe has the characteristics of single selective recognition, high sensitivity and low detection limit (0.18 mu M) on divalent palladium, and the fluorescence intensity of the fluorescent probe and the concentration of divalent palladium are in a good linear relationship within the range of 0-40 mu M. Meanwhile, an application experiment verifies that when the fluorescent probe is used for detecting the divalent palladium in the traditional Chinese medicinal materials, the adding standard recovery rate ranges from 90.8% to 106.4%. Therefore, the fluorescent probe disclosed by the invention has a wide application prospect in the fields of bivalent palladium detection reagents and rapid detection of heavy metals in traditional Chinese medicinal materials.

The invention discloses a method for preparing a polyfluoroalkyl coumarin derivative, and belongs to the field of organic synthesis. According to the method, cheap and easily available polyfluorocarboxylic acid anhydride is used as a polyfluoroalkylating reagent, and in-situ activation of NHPI is combined to prepare the C3-site polyfluoroalkyl substituted coumarin derivative. Under the condition of visible light catalysis, polyfluoroalkyl carboxylic acid anhydride is used as a polyfluoroalkylating reagent, polyfluoroalkyl free radicals are generated through in-situ activation of NHPI, the free radicals and aromatic propiolate are subjected to a free radical cyclization rearrangement reaction, and finally preparation of the C3-site polyfluoroalkyl substituted coumarin derivative is achieved. The polyfluoroalkyl carboxylic acid anhydride used in the method is stable in property, low in price and easy to obtain, and the synthesis cost is reduced. The method is wide in applicable substrate range and applicable to various polyfluoroalkyl carboxylic acid anhydrides, and the tolerance of reaction functional groups is good.

The application discloses a method for preparing aromatic benzyl propargyl ketone by light induction and biological application, belongs to the technical field of organic synthesis and biological medicine, and converts aromatic benzyl propargyl alcohol into aromatic benzyl propargyl ketone under the condition of light induction; the change of the functional group before and after light induction is that the hydroxyl alkyne without reaction activity is converted into the carbonyl alkyne with click reaction activity, fluorescence enhancement can be realized, and the method can be used for imaging and tracing; and the aromatic benzyl propargyl ketone can react with a compound containing an amino group or a biological macromolecule to realize the killing of tumor cells. The method uses light as a starting switch, the reaction condition is simple, controllability is good, no additional catalyst is needed, and the method is easy to mass-produce, so the method has wide application prospects in polypeptide or protein labeling, anti-tumor and the like.

The invention discloses a method for preparing propargyl ester through 1, 3-enyne 1, 2-carbon esterification reaction based on a polarity matching strategy and application, and the method comprises the following steps: in the presence of a copper catalyst, a ligand and tert-butyl peroxybenzoate and under the heating condition, reacting a compound in a formula (1) with a compound in a formula (2) in an organic solvent to generate the propargyl ester in a formula (3). The preparation method provided by the invention can be suitable for alkyl-substituted 1, 3-enyne, aryl-substituted 1, 3-enyne, silicon-substituted 1, 3-enyne, an electron-rich C-H substrate, an electron-deficient C-H substrate, a Si-H substrate and a Ge-H substrate, and has the advantages that the substrates are simple and easy to obtain, and the universality is wide. The preparation method provided by the invention has the advantages of cheap and easily available reaction raw materials, simple reaction operation, wide application range of reaction substrates, easy amplification of reaction, mild reaction conditions and the like, and can realize industrial production and application.

The present invention relates to a compound of formula (I) wherein n is 1 or 2, R1 is halogen, (C1-C4) alkyl, halo (C1-C4) alkyl, (C1-C4) alkoxy, halo (C1-C4) alkoxy, ethynyl, propargyl, or (C3-C6) cycloalkyl, or two R1 form a cyclopentane ring fused to phenol; r2 and R3 represent H, cyano, ethynyl, propargyl, (C1-C4) alkyl, hydroxy (C1-C4) alkyl, or halogenated (C1-C4) alkyl, or R2 and R3 together with the atoms linking them form a (C5-C6) carbocyclic ring fused to the pyridazine ring; r4 and R5 together with the N to which they are attached form an optionally substituted 3-7 membered monocyclic heterocycloalkyl ring, 8-11 membered bicyclic heterocycloalkyl ring or 7-12 membered bicyclic heterocyclic spiro ring. The invention also relates to a medicament and a pharmaceutical composition comprising said compounds of formula (I) and to their therapeutic use, in particular as inhibitors of NOD-like receptor protein 3 inflammasome for the treatment of e.g. Parkinson's disease or frontotemporal dementia.

The invention belongs to the technical field of biomedical materials and tumor treatment, and discloses a biological orthogonal catalytic microneedle based on a cytotoxic polyethyleneimine matrix as well as a preparation method and application of the biological orthogonal catalytic microneedle. The microneedle patch comprises a backing layer and a microneedle array, wherein the microneedle array is formed by mixing polyvinyl alcohol (PVA) loaded with metal nanoparticles and polyethyleneimine (PEI) with a hydrogel matrix. According to the invention, the inherent cytotoxicity (membrane destroying ability) of PEI is creatively combined with the catalytic activity of a metal catalyst (such as palladium) to construct a synergistic treatment system which turns toxins into treasures. The PEI matrix has dual functions in the microneedle: on one hand, the PEI matrix is used as a potent ligand to anchor and stabilize the metal nanoparticles and prevent the metal nanoparticles from leaking; on the other hand, as a therapeutic agent, tumor cell membranes are destroyed through electrostatic interaction. The microneedle patch is activated by catalyzing a prodrug (such as doxorubicin protected by propargyloxycarbonyl) in situ, meanwhile, the physical membrane destruction effect of PEI is utilized, the synergistic anti-tumor effect of physical destruction and chemical killing is achieved, and the treatment efficiency of superficial tumors such as melanoma is remarkably improved.

The present application relates to a kind of biological ortho prodrug, composition and its application, specifically disclose a kind of drug prodrug with substituted acrylamide or substituted vinyl sulfonamide structure, is obtained by the reaction of covalent warhead comprising active drug and N-alkyl hydroxylamine.The drug prodrug can be released by Retro-Cope elimination reaction and Cope elimination reaction with tension alkyne, and the release rate can reach more than 90%, to realize on-demand activation active warhead, effectively solve the off-target problem of covalent inhibitor.In addition, by introducing the drug or fluorophore containing hydroxyl / amine group in the propargyl position of tension alkyne, the intermediate produced after Cope elimination reaction of tension alkyne can further undergo elimination reaction, release the drug or fluorophore containing hydroxyl / amine group, realize combined therapy or real-time monitoring of drug release.The above-mentioned drug prodrug and the composition formed by the combination of tension alkyne have good application prospect in the preparation of drug delivery system or active drug.

The invention belongs to the technical field of chemical synthesis, and particularly relates to a method for chiral resolution of a clodinafop-propargyl enantiomer. According to the present invention, the high performance liquid chromatography-mass spectrometry technology is adopted to separate the clodinafop-propargyl enantiomer, the chromatographic column is the polysaccharide derivative chiral chromatographic column, the mobile phase A is the organic solvent, the mobile phase B is pure water, the volume ratio of the mobile phase A to the mobile phase B is 40: 60-100: 0, isocratic elution is performed, the column temperature is 30-35 DEG C, and the flow rate is 0.5-0.8 mL / min. The invention provides the method for effectively separating the chiral propargyl enantiomer, and the method has the advantages of high sensitivity, simplicity in operation, high separation speed and the like.

Battery comprising an electrolyte and a negative electrode; wherein the electrolyte comprises an additive B with a structure of formula I: where R1, R2 and R3 are independently of -H or -C p H 2p+1 are selected, where 1 ≤ p ≤ 4; wherein R4, R5 and R6 are independently composed of a vinyl group, allyl group, oxyvinyl group, oxyallyl group, oxyallyl group, ethinyl group, propargyl group, oxyethynyl group or are selected oxypropargyl group; where R7, R8 and R9 are independently selected from -H, -CH3 or -CH2CH3; wherein the negative electrode has an active material layer of the negative electrode; where the powder conductivity of the active material layer of the negative electrode is a in units of S / cm; where the mass fraction of additive B is b% relative to the mass of the electrolyte, and a and b fulfill the following relationship: 6.5 ≤ a / b ≤ 550.

The application discloses a powder back fern acid derivative containing a 1,2,3-triazole group and a preparation method and application thereof, and belongs to the field of pharmaceutical chemical industry. The powder back fern acid is used as a substrate, first reacts with propargylamine under the action of a condensing agent to obtain an intermediate N-propargyl powder back fern amide, then undergoes a click reaction with an azide compound to synthesize a series of powder back fern acid derivatives containing a 1,2,3-triazole. The powder back fern acid derivatives obtained are tested for cytotoxicity on five common cancer cell lines. The results show that most of the compounds exhibit obvious anti-proliferation activity on the five cancer cell lines, and meanwhile, some of the compounds can reach more than half of the inhibition rate on the five cancer cell lines at a concentration of 10 muM. The synthesis process is simple and fast, and the synthesis efficiency is high. The application is another effective way for synthesizing new compounds by modifying the structure of the powder back fern acid after amination. The powder back fern acid derivatives prepared by synthesis are expected to be applied in the field of antitumor drugs.

The utility model discloses a kind of catalyst filtering devices suitable for clomazone synthesis, specifically related to filter equipment technical field, including cylinder, be located in the inlet pipe of cylinder top surface and be located in the outlet pipe of cylinder bottom surface, the inside of the cylinder is equipped with three mounting frames, and the inside of three mounting frames is equipped with the filter plate for clomazone synthesis catalyst filtering, the inside both sides of mounting frame are fixedly installed with plug-in block.The utility model discloses a kind of catalyst filtering devices suitable for clomazone synthesis, in actual work, staff will arm through processing mouth and enter the inside of cylinder, and push two dials to move in the way of mutually far away, limit rod can be pulled out from the limiting hole of filter plate, and then filter plate can be extracted from the inside of mounting frame, new filter plate is inserted into mounting frame through processing mouth, the quick replacement of filter plate can be completed, to effectively avoid the influence of filtering efficiency due to the slow filter plate replacement speed.

The invention discloses a high-corrosion-resistance bright chemical nickel plating solution and an integrated circuit nickel plating process, and relates to the field of the electronic core industry. The high-corrosion-resistance bright chemical nickel plating solution comprises a water-soluble nickel salt, boric acid, sodium citrate, malic acid, N, N-dimethyl formamide and a solvent. According to the present invention, the water-soluble nickel salt, the boric acid, the sodium citrate, the malic acid, the N, N '-bis (2-ethoxyl) ethylenediamine, the N, N-diethyl propargyl amine formate, the saccharin sodium salt and the reducing agent are co-matched so as to easily refine nickel crystal grains and promote the uniform deposition of the nickel crystal grains, such that the nickel crystal grains can be uniformly dispersed, and the nickel crystal grains can be uniformly dispersed; according to the invention, the brightening of the plating layer can be realized, the porosity of the plating layer is reduced, and the permeation of a corrosive medium is favorably blocked, so that the corrosion resistance of the integrated circuit substrate is improved.

The application discloses a preparation method of 4-bromothieno[2,3-c]pyridine-2-carboxylic acid ethyl ester, which comprises the following steps: 5-bromo-4-iodopyridine-3-thiol and propargyl acid ethyl ester are subjected to a Sonogashira coupling and a ring-closing series reaction under the action of a catalyst and an alkali to obtain 4-bromothieno[2,3-c]pyridine-2-carboxylic acid ethyl ester. The raw material adopted by the method is cheap and easy to obtain, the synthesis method is simple to operate, the reaction condition is mild, the requirement for equipment is low, and the method is suitable for the needs of industrial large-scale production.

The invention relates to the field of preparation of insect sex pheromone, in particular to a preparation method of insect sex pheromone (8E, 10E)-dodecadiene-1-alcohol. The method comprises the following steps: in an N2 atmosphere, carrying out a reaction on p-toluenesulfonic acid propargyl ester and HML (zirconocene hydrogen chloride), under the action of Pd (Ph3P) 2Cl2 and R2AlH (2), carrying out a reaction with (E)-halogenated propylene (1) to prepare an intermediate (I), carrying out a reaction on the intermediate (I) and a Grignard reagent (3), and carrying out hydrolysis to prepare the insect sex pheromone (8E, 10E)-dodecadiene-1-alcohol. The method disclosed by the invention is mild in reaction condition, simple in post-treatment, environment-friendly, high in product yield, good in stereoselectivity and suitable for industrial production.

The present invention relates to a non-aqueous electrolyte and a lithium secondary battery comprising same. The non-aqueous electrolyte comprises a lithium salt, an organic solvent, and an additive, the additive comprising a first additive and a second additive, wherein the first additive comprises a compound in which two cyclic sulfur oxide groups are bonded directly or via a linker, and the second additive comprises a nitrogen-containing heteroaromatic compound substituted with at least one of a vinyl group and a propargyl group.

The present application relates to a kind of morpholine ring compound and derivative and preparation method and application.The morpholine ring compound is the compound with the structure shown in formula A or formula B, or their enantiomers.The present application starts from ethynyl carbonate and 4-amino dienone or N-benzyl oxetane-3-amine, develops a continuous asymmetric propargyl amination and desymmetrization Michael addition reaction using cuprous iodide and chiral pyridine oxazoline ligand as catalyst, and desymmetrization ring-opening reaction of butylene oxide with diphenyl phosphate, efficiently, with high enantioselectivity and excellent diastereoselectivity Synthesis of multiple quaternary carbon center and multifunctional morpholine ring derivatives and nitrogen-containing adjacent quaternary carbon and hydroxyl-containing morpholine derivatives;And further develop a derivative with antitumor activity.