2-(2-溴乙基)苯甲醛置于盐酸,Sodium Hydride,Copper(II) Sulfate体系中,用 四氢呋喃,1,4-二氧六环,甲醇,乙醚,二氯甲烷,甲苯,Mineral Oil 用作溶剂,化学反应 24.0H,反应生成(S)-1-苯基-1,2,3,4-四氢异喹啉 参考文献:Stereoselective Total Syntheses Of Solifenacin And N-Acetyl-1-(4-Chlorophenyl)-6,7-Dimethoxytetrahydroisoquinoline 标题:Stereoselective Total Syntheses Of Solifenacin And N-Acetyl-1-(4-Chlorophenyl)-6,7-Dimethoxytetrahydroisoquinoline 摘要:A Highly Stereoselective Synthesis Of 1-Aryl-1,2,3,4-Tetrahydroisoquinoline Drugs Such As Solefinacin (Muscarinic Acetylcholine Receptor Antagonist) And N-Acetyl-1-(4-Chlorophenyl)-6,7-Dimethoxytetrahydroisoquinoline (Ampa Receptor Antagonist) Has Been Accomplished Using (R)-Tert-Butanesulfinamide As A Chiral Source. Chiral Tetrahydroisoquinolines Have Been Prepared Through The Aryl Grignard Addition To Chiral N-Sulfinylimines Followed By Haloamide Cyclization. Doi:10.1055/s-0034-1378515
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-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.
专利号:WO-2008120080-A2 优先权日:2007-03-30 标 题:An improved process for the synthesis of solifenacin
专利号:CN-107540606-A 优先权日:2016-06-29 标题 :A kind of method of bidirectional enantioselective synthesis of chiral tetrahydroisoquinoline catalyzed by iridium
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:Pollegioni, L.; Molla, G., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 3, 251.