56 results about "Drug synthesis" patented technology

The invention belongs to the technical field of drug synthesis, and particularly relates to an adamantane derivative as well as a synthesis method and application thereof. The adamantane derivative comprises an intermediate structural formula I, an intermediate structural formula II and an intermediate structural formula III, and the structural general formula is as follows: Linker is substituted or unsubstituted C6-C10 aroyl, R1 is hydrogen or C1-C6 alkyl, R2 is hydrogen, C1-C6 alkyl or a nitrogen-containing or nitrogen-free structural fragment, or the integral structure of R1R2 is N-substituted heterocyclic pentyl or heterocyclic cyclohexyl. According to the adamantane derivative provided by the invention, an adamantane structure is combined with part of groups of OAB-14, and a parent nucleus structure is changed, so that the drug activity is improved. The invention also provides a synthesis method of the compound, the obtained compound is screened through cell viability research, and the compound has a potential synergistic effect in the aspects of preventing influenza and treating Alzheimer's disease.

The invention relates to a synthesis method of milobalin or acid salt thereof, and belongs to the technical field of medicine synthesis. In order to solve the problem that chiral resolution needs to be adopted in the prior art, the invention provides a synthesis method of miloabalin or an acid salt thereof, which comprises the following steps: under the action of an organic strong base, carrying out Michael addition reaction on a compound shown as a formula III and acetonitrile in a non-polar organic solvent at a low temperature of-50 DEG C or below to obtain an intermediate product; under the alkaline condition, the intermediate product is subjected to an oxidation reaction and a hydrolysis reaction under the action of an oxidizing agent, after the reaction is finished, an intermediate product is obtained through acidification, and the intermediate product is subjected to a high-temperature decarboxylation reaction in an aprotic solvent to obtain a compound of a formula VI; and carrying out Hofmann degradation reaction on the compound of formula VI to obtain the compound of formula I miloabalin or miloabalin acid salt. The method has the advantages of high stereoselectivity, no need of chiral resolution operation, avoidance of the problem of large material loss caused by resolution, high chiral purity and high yield.

The invention discloses a 7-azaindole compound as well as a preparation method and application thereof, belongs to the field of medicine synthesis, and particularly relates to a pyrazole or indole substituted 7-azaindole compound as shown in a general formula (I) as well as a preparation method and application thereof in medicine. According to the compound disclosed by the invention, tumor cachexia skeletal muscle atrophy is relieved by inhibiting ActRIIB protein in an MSTN pathway, and a remarkable tumor cachexia resisting effect is achieved. Experimental results show that the compound has good anti-cachexia activity and can be further used for preparing novel anti-cachexia drugs. # imgabs0 #

The invention belongs to the technical field of medicine synthesis, and particularly relates to a memantine derivative and a synthesis method and application thereof. The memantine derivative comprises an intermediate structural formula I, an intermediate structural formula II, an intermediate structural formula III and a structural general formula, Linker is substituted or unsubstituted C6-C10 aroyl, R1 is hydrogen or C1-C6 alkyl, R2 is hydrogen, C1-C6 alkyl or a nitrogen-containing or nitrogen-free structural fragment, or the integral structure of R1 and R2 is N-substituted heterocyclic pentyl or heterocyclic cyclohexyl. According to the memantine derivative provided by the invention, a memantine group is combined with an OAB-14 partial structure to change a parent nucleus structure, so that the drug activity is improved. The invention also provides a synthesis method of the compound, and the obtained compound is used for treating Alzheimer's disease and Parkinson's disease.

The application relates to a synthesis method of an anti-freezing glycopeptide polypeptide and belongs to the technical field of polypeptide drug synthesis. The method comprises the following steps: 2-CL-Resin is used as a carrier resin, under the condition of adding an activating agent, the carrier resin and alanine are coupled to obtain Fmoc-Ala-2-CL-Resin; according to the amino acid sequence of the anti-freezing glycopeptide, other amino acids are sequentially coupled through a solid-phase synthesis method; after a protecting group is removed and the carrier resin is cleaved, the anti-freezing glycopeptide crude peptide is obtained; and after purification, salt conversion and freeze-drying, the anti-freezing glycopeptide polypeptide is obtained. The method has the advantages of short synthesis period, low cost, easy post-treatment, few by-products, high product yield, facilitation of large-scale production of the anti-freezing glycopeptide, and considerable economic applicative value and wide application prospect.

Embodiments of the present application provide a three-dimensional molecular structure generation method, device, equipment and storage medium, at least applied to the field of artificial intelligence and the field of drug synthesis, wherein the method comprises: obtaining atomic type noise and atomic coordinate noise at a current time step; constructing a full connection adjacency matrix based on the atomic type noise; performing three-dimensional isometry processing on the atomic type noise, the atomic coordinate noise and the full connection adjacency matrix to obtain a molecular structure distribution average value at the current time step; generating a molecular structure of the molecule iteratively based on the molecular structure distribution average value at the current time step to obtain a molecular representation of the molecule; and constructing the three-dimensional molecular structure through the molecular representation. Through the present application, the efficiency of three-dimensional molecular structure generation can be accelerated and cumulative errors can be avoided, so as to accurately generate a three-dimensional molecular structure of an effective molecule.

This invention belongs to the technical field of chemical drug synthesis, specifically relating to an indole alkaloid compound, its preparation method, and its application. The indole alkaloid compound, whose structural formula is shown in Formula I, is synthesized from 7-bromoindole and a boric acid ester as starting materials. The preparation process is simple and easy, and the resulting indole alkaloid compound or a pharmaceutically acceptable salt thereof exhibits highly effective targeted inhibition of STEAP1, inhibiting STEAP1 at both the protein and cellular levels and demonstrating potent anti-proliferative effects against prostate cancer cells in animals.

This invention belongs to the field of pharmaceutical synthesis technology, specifically relating to a diarylurea derivative, its preparation method, and its application. The diarylurea derivative of this invention is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, which exhibits high inhibitory activity against wild-type (WT), mutant G595R, and G667C tropomyosin receptor kinase (TRK), and can be used to treat NTRK fusion-positive locally advanced or metastatic solid tumors.

The invention discloses ketoreductase with stereoselective reduction activity and application of the ketoreductase, and belongs to the technical field of medicines, the amino acid sequence of the ketoreductase is shown as SEQ ID NO: 1, SEQ ID NO: 2 or SEQ ID NO: 3; according to the method, racemic nebivolol chloroketone is taken as an initiator, an R-configuration ketone substrate is recognized through the ketoreductase and is reduced into optically pure alcohol (R, R-2), meanwhile, a configuration S-configuration substrate is split, and a simple and efficient preparation method with high atom economy is provided for an optically pure intermediate necessary for nebivolol drug synthesis.

This invention belongs to the technical field of drug synthesis, specifically relating to memantine derivatives, their synthetic methods, and applications. The memantine derivatives include intermediate structural formulas I, II, and III, as well as a general structural formula. The linker is a substituted or unsubstituted C6-C10 aryl group, R1 is hydrogen or a C1-C6 alkyl group, and R2 is hydrogen, a C1-C6 alkyl group, or a nitrogen-containing or nitrogen-free structural fragment, or the overall structure of R1 and R2 is an N-substituted heterocyclopentyl or heterocyclohexyl group. The memantine derivatives provided by this invention improve drug activity by combining the memantine group with the OAB-14 partial structure, thereby altering the core structure. This invention also provides a synthetic method for the obtained compounds used in the treatment of Alzheimer's disease and Parkinson's disease.