专利号:US-11479577-B2 优先权日:2016-05-18 标题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY; DAVIES IEUAN; OTTER CARL; BATCHELOR RHYS 权利人:NZP UK LTD 摘要:The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):wherein:, R1, R2, R3, R4, R5, R6 and Y are as defined herein.The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.
专利号:WO-2024218783-A1 优先权日:2023-04-17 标题 :Green chemistry approach for synthesis of mavacamten and its intermediate using novel methodology 发明人:CHEEPIRISHETTI SHANKAR; CHEEPIRISHETTI ASHRIT; KOMARRAJ SNEHITHA; KAUSHAL KISHORE; BORREDDY SIVA PRASAD REDDY; BASANTHI DEVI; SHAIK SAYYAD SHAMSHUDDIN; KUMAR MUKES 权利人:DASHA PHARMACEUTICALS PRIVATE LTD 摘要:The present invention discloses a green chemistry approach for synthesis of Mavacamten (Compound of formula I). The present invention also discloses a novel process for preparation of an intermediate 1-isopropylpyrimidine-2,4,6(1H,3H,5H)-trione (Compound of formula VII) and further preparation of Mavacamten using this intermediate, following novel methodology.
专利号:US-4713479-A 优先权日:1986-11-28 标题 :Synthesis of high-purity dialkyl 2-vinylcyclopropane-1,1-dicarboxylate 发明人:CLARK JR CLARENCE E; FAYTER JR RICHARD G 权利人:NAT DISTILLERS CHEM CORP 摘要:This invention relates to a two-step synthesis of high purity dialkyl 2-vinyl-cyclopropane-1,1-dicarboxylate in which a mixture of trans- and cis-1,4-dihalobutene-2 is first isomerized to essentially trans-1,4-dihalobutene-2 followed immediately by cyclocondensing the resultant trans-1,4-dihalobutene-2 with a malonic ester in the presence of an alcoholic solution of a metallic alkoxide.
专利号:US-8076479-B2 优先权日:2006-08-28 标题 :Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivatives and intermediates 发明人:CHEN FRANK XING; KEERTIKAR KARTIK M; KUO SHEN-CHUN; LEE HONG-CHANG; RAGHAVAN RAMANI R; WU GEORGE G; XIE JI 权利人:CHEN FRANK XING; KEERTIKAR KARTIK M; KUO SHEN-CHUN; LEE HONG-CHANG; RAGHAVAN RAMANI R; WU GEORGE G; XIE JI; SCHERING CORP 摘要:Disclosed is a process for the synthesis of compounds of Formula I n nby sequentially aminating, first with a primary amine and then with a secondary amine, an intermediate compound of the structure of Formula E1,n n nwherein R 1 is a linear, branched, or cyclic alkyloxy functional group of the structure (—R 2a —OH), R 2a is a linear, branched or cyclic alkyl group, R 2 is a linear, branched or cyclic alkyl group, and R 3 is an alkylene-heterocycle, said process comprising forming intermediate compound of Formula E1 by reacting, in a refluxing reaction solvent selected from alcohols having 5 or less carbon atoms and mixtures of two or more thereof, a methanol solution of a salt of a 4-alkyl-3-amino-pyrazole compound of Formula C1,n n nwith a diamidization reagent selected from dimethylmalonate, monomethylmalonyl-chloride, and malonyl dichloride in the presence of a Lewis base having sufficient proton affinity to abstract a proton from the 1-position nitrogen on the pyrazole ring.
专利号:US-4866175-A 优先权日:1966-11-08 标 题 :Novel process for the synthesis of quinoxaline and benzimidazole-N-oxides 发明人:ISSIDORIDES COSTAS H; HADDADIN MAKHLUF J 权利人:RESEARCH CORP 摘要:The synthesis of quinoxaline and benzimidazole-N-oxides and of ester amd amide derivatives of 3-hydroxy-2-quinoxalinecarboxylic acid by a movel process consisting of the reaction between a benzofuroxan and an activated methylene-containing compound under basic conditions.
专利号:US-4092351-A 优先权日:1976-02-17 标 题 :Method of synthesis of 4,5,6-trihydroxyisophthalic acid 发明人:SHIPCHANDLER MOHAMMED T 权利人:IMC CHEMICAL GROUP 摘要:A process for the synthesis of 4,5,6-trihydroxyisophthalic acid by reacting dialkyl glutarate with dialkyl dialkoxymalonate.
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合成参考文献
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