合成目标产物 Solifenacin 主要起始原料 Ethyl (S)-1-Phenyl-1,2,3,4-Tetrahydro-2-Isoquinolinecarboxylate And (R)-(-)-3-Quinuclidinol
118864-75-8 = 242478-37-1 + 732228-02-3 反应条件:1.1R:Et3N,S:Phme,30 Min,5-30°C; 30 Min,25-30°C2.1R:Nah,S:Phme,25-30°C; 20 H,110-115°C; 115°C -> 25°C2.2R:H2O,20-30°C 标题:An Improved Process For The Preparation Of Highly Pure Solifenacin Succinate Via Resolution Through Diastereomeric Crystallization 作者:By Trinadhachari,Ganala Naga Et Al 参考文献:Organic Process Research & Development 日期:2014 卷标:18(8) 页码:934-940
索利那新盐酸盐置于碳酸氢钠体系中,用 水,乙酸乙酯 用作溶剂,化学反应生成索非那新 参考文献: Process For Preparing Chemically And Chirally Pure Solifenacin Base And Its Salts[fr] Procédé De Préparation D'Une Solifénacine Base De Pureté Chimique Et De Pureté Chirale Et De Ses Sels 标题: Process For Preparing Chemically And Chirally Pure Solifenacin Base And Its Salts[fr] Procédé De Préparation D'Une Solifénacine Base De Pureté Chimique Et De Pureté Chirale Et De Ses Sels 摘要:本发明提供了改进的制备化学纯和对映纯索利那辛碱的方法.本发明还提供了一种含有至少98%纯度的索利那辛盐的组合物.本发明还披露了索利那辛的某些新盐以及索利那辛盐酸盐和索利那辛草酸盐的新多形态,均为纯形式.
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.
参考标题:Engineering An Enantioselective Amine Oxidase For The Synthesis Of Pharmaceutical Building Blocks And Alkaloid Natural Products 作者:Diego Ghislieri,Anthony P. Green,Marta Pontini,Simon C. Willies,Ian Rowles,Annika Frank,Gideon Grogan,Nicholas J. Turner |发布日期:2013.7.24 摘要:Catalytic Methods For The Production Of Enantiomerically Pure Chiral Amines Is A Key Challenge Facing The Pharmaceutical And Fine Chemical Industries. This Challenge Is Highlighted By The Estimate That 40-45% Of Drug Candidates Contain A Chiral Amine, Fueling A Demand For Broadly Applicable Synthetic Methods That Deliver Target Structures In High Yield And Enantiomeric Excess. Herein We Describe The Development
合成参考文献
摘要:Morales-Olivas FJ, Estañ L. Solifenacin pharmacology. Arch Esp Urol. 2010 Jan;63(1):43–52. 参考文献:10.1155/2011/714978 摘要:Masumori N, Miyamoto S, Tsukamoto T, Furuya S, Iwasawa A, Sato T, Itoh N, Shibuya A, Oda T. The efficacy and safety of propiverine hydrochloride in patients with overactive bladder symptoms who poorly responded to previous anticholinergic agents. Adv Urol. 2011;2011():714978. 参考文献:10.4111/kju.2011.52.6.396 摘要:Han YK, Lee WK, Lee SH, Yang DY, Kim H. Effect of desmopressin with anticholinergics in female patients with overactive bladder. Korean J Urol. 2011 Jun;52(6):396–400.