(R)-Quinuclidin-3-Yl Phenethylcarbamate置于硫酸,溶剂黄146体系中,用 乙醇,乙酸乙酯 用作溶剂,化学反应 8.0H,反应生成琥珀酸索利那辛 参考文献: Process For The Preparation Of Solifenacin And Salts Thereof[fr] Procédé D'élaboration De Solifénacine Et De Sels De Solifénacine 标题: Process For The Preparation Of Solifenacin And Salts Thereof[fr] Procédé D'élaboration De Solifénacine Et De Sels De Solifénacine 摘要:该发明提供了一种制备索利那辛或其药用可接受的酸盐的新工艺,包括在酸的存在下将(R)-喹诺啉-3-基苯乙基氨甲酸酯与苯甲醛反应,以获得一个对映异构体混合物(S,R)-((R)-喹诺啉-3-基) 1-苯基-3,4-二氢异喹啉-2(1 H)-羧酸酯的公式(Iv),该混合物可以被分离,然后可以回收索利那辛或其药用可接受的酸盐.该发明还提供了参与该工艺的新关键中间体(R)-喹诺啉-3-基苯乙基氨甲酸酯.此外,该发明提供了一种将(R)-((R)-喹诺啉-3-基) 1-苯基-3,4-二氢异喹啉-2(1 H)-羧酸酯转化为一个对映异构体混合物(S,R)-((R)-喹诺啉-3-基) 1-苯基-3,4-二氢异喹啉-2(1 H)-羧酸酯的方法.
专利号:US-12098126-B2 优先权日:2021-08-23 标题:Methods of iron catalyzed C-H bond amination 发明人:CHE CHI-MING; YOU TINGJIE 权利人:VERSITECH LTD; LABORATORY FOR SYNTHETIC CHEMISTRY AND CHEMICAL BIOLOGY LTD 摘要:Described herein is an iron(II)-phthalocyanine catalyzed C—H bond amination of alkyl azides. The catalyst is effective to produce intramolecular amination of saturated C—H bonds in moderate to excellent yields and the methods are tolerant of a wide scope of substrates. The methods described are useful for the synthesis of natural products derivatives and for the late-stage functionalization of pharmaceuticals.
专利号:US-7741489-B2 优先权日:2007-03-30 标题:Process for the synthesis of solifenacin 发明人:PUIG SERRANO JORDI; CAMPS PELAYO 权利人:MEDICHEM SA 摘要:The present invention provides an improved synthetic strategy for the preparation of solifenacin and pharmaceutically acceptable salts thereof.
专利号:US-2011077405-A1 优先权日:2008-05-23 标题:Process for preparation of enantiomerically pure (s)-1-phenyi-1,2,3,4- tetrahydroisoquinoline 发明人:ZEGROCKA-STENDEL OLIWIA; ZAGRODZKA JOANNA; LASZCZ MARTA 权利人:ZEGROCKA-STENDEL OLIWIA; ZAGRODZKA JOANNA; LASZCZ MARTA 摘要:Process for preparation of (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline wherein 1-phenyl-1,2,3,4-tetrahydroisoquinoline is reacted with D-(−)-tartaric acid in a solvent system comprising of methanol and water, preferably at 3.3:1 to 1:1 volume ratio, the crystallization mixture is left for crystallization and (S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline is released from obtained crystalline diastereoisomeric salt according to standard procedures. (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline is the intermediate in enantiomeric synthesis of solifenacin.
专利号:US-9982006-B2 优先权日:2014-08-21 标题:2′-chloro aminopyrimidinone and pyrimidine dione nucleosides 发明人:CLARKE MICHAEL O'NEIL HANRAHAN; MACKMAN RICHARD L; SIEGEL DUSTIN 权利人:GILEAD SCIENCES INC 摘要:Provided herein are formulations, methods and substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted 2′-chloro aminopyrimidinone and pyrimidine dione compounds.
专利号:US-2009326230-A1 优先权日:2006-07-19 标题 :Process for preparing solifenacin and its salts 发明人:MATHAD VIJAYAVITTHAL THIPPANNACHAR; LILAKAR JAYDEEPKUMAR DAHYABHAI; GILLA GOVERDHAN; KIKKURU SRIRAMIREDDY; CHINTA RAVEENDRA REDDY; DUDIPALA SWAROOPA 权利人:REDDYS LAB LTD DR; REDDYS LAB INC DR 摘要:The present invention relates to solifenacin in solid form and a process for its preparation and to a process for the preparation of (1S)-1-Phenyl-1,2,3,4-tetrahydro-isoquinoline, a key intermediate in the synthesis of solifenacin and its salts.
专利号:US-2010029944-A1 优先权日:2006-11-22 标题:Process for the Synthesis of Solifenacin 发明人:PUIG JORDI; SANCHEZ LAURA; MASLLORENS ESTER; AUGER IGNASI; BOSCH JORDI 权利人:CORPORACION MEDICHEM S L 摘要:This invention provides improved methods for making solifenacin and pharmaceutically acceptable salts thereof. The instant methods are unexpectedly advantageous in their simplicity and efficiency.
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