专利号:WO-2023031841-A1 优先权日:2021-09-03 标题:A process for the stereospecific synthesis of vitamin k2 and its intermediates 发明人:MEHTA DILIP; SHASHTRI MAYANK; RAJU BNS; VORA PARIN; MAHALE UMAKANT 权利人:SYNERGIA LIFE SCIENCES PVT LTD 摘要:The present disclosure relates to a novel process for the synthesis of stereospecific compounds of Vitamin K2 group in general and Vitamin K2-7, in particular. It also discloses novel intermediates useful in the synthesis of stereospecific Vitamin K2-7. Compounds of the Vitamin K2 group obtained are crystalline and exhibit well defined melting points.
专利号:US-5668285-A 优先权日:1986-10-31 标 题 :Total synthesis of northebaine, normophine, noroxymorphone enantiomers and derivatives via N-Nor intermediates 发明人:RICE KENNER CRALLE; NEWMAN AMY HAUCK 权利人:US HEALTH 摘要:The invention involves a method of making key intermediates useful in the synthesis of many opiate narcotics and antagonists and agonists; and the non-opiate enantiomers thereof which have potent antitussive properties. The synthesis starts from either the natural or unnatural enantiomer of nordihydrocodeinone and produces 8, 14-dihydronorthebaine, the diketal of 7-bromonordihydrocodeinone, northebaine, norcodeinone diketal and 14-hydroxynorcodeinone intermediates without the necessity of leaving the N-nor structure. The syntheses have fewer steps than previous methods, and also have high yields.
专利号:WO-2019202611-A1 优先权日:2018-04-21 标题:An improved process for the synthesis of ivabradine and its pharmaceutically acceptable salts 发明人:NANDEPU Venkateswara Rao; BOPPANA DURGA PRASAD 权利人:METROCHEM API PVT 摘要:: Disclosed herein is an improved process for the preparation of Ivabradine and pharmaceutically acceptable salts thereof. The invention more particularly disclosesthe synthesis of key intermediates viz.,(S)-N-[(4,5-dimethoxybenzocydobut-l-yl)-methyl]-N- (methyl)amine hydrochloride of Formula-II and 3-(3-Iodopropyl)-7,8-dimethoxy-1,3-dihydro-2H-3-benzapin-2-one of Formula-III, and its use in industrial synthesis of Ivabradine and pharmaceutically acceptable salts thereof.
专利号:WO-2011101864-A1 优先权日:2010-02-17 标题 :Novel process for the synthesis of phenoxyethyl derivatives 发明人:JAIN RAJESH; JAGDEESHWAR RAO R; MAHENDER RAO SIRIPRAGADA 权利人:PANACEA BIOTEC LTD; JAIN RAJESH; JAGDEESHWAR RAO R; MAHENDER RAO SIRIPRAGADA 摘要:The present invention provides an improved process for the synthesis of 2-[2- (2,2,2-trifluoroethoxy)phenoxy]ethanol intermediate, its derivatives and/or its pharmaceutically acceptable salts, useful in the synthesis of α-1 adrenoceptor blockers such as silodosin.
专利号:WO-03031376-A1 优先权日:2001-10-12 标 题 :Solid phase synthesis of substituted 1,5-benzodiazepine-2-one and 1,5-benzothiazepine-2-one 发明人:MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 权利人:AVENTIS PHARMA INC; MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 摘要:A solid phase synthetic method for making substituted 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one. The method is useful for synthesis of large numbers of compounds through automated parallel synthesis or combinatorial library generation and is thus important to rapid discovery or new therapeutic agents containing the base structure of 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one.
专利号:US-8357819-B2 优先权日:2007-05-11 标 题 :Method for the synthesis of (Z)-3-[2-butoxy-3′-(3-heptyl-1-methyl-ureido)-biphenyl-4-yl]-2-methoxy-acrylic acid 发明人:BOITEAU JEAN-GUY 权利人:GALDERMA RES & DEV; BOITEAU JEAN-GUY 摘要:The invention relates to a process for the synthesis of (Z)-3-[2-butoxy-3′-(3-heptyl-1-methylureido)biphenyl-4-yl]-2-methoxyacrylic acid of formula (I): n nand also to the process for the synthesis of the reaction intermediates of general formula (XII), and to the said compounds when R2 is chosen from the methyl, trifluoromethyl, phenyl and 4-tolyl radicals: