2-(2-溴乙基)苯甲醛置于盐酸,Sodium Hydride,Copper(II) Sulfate,三乙胺体系中,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 25.17H,反应生成(S)-1-苯基-1,2,3,4-四氢-2-异喹啉甲酸乙酯 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:US-2008242697-A1 优先权日:2007-03-30 标题 :Process for the synthesis of solifenacin
参考标题:Enantioselective Iridium-Catalyzed Hydrogenation Of 1- And 3-Substituted Isoquinolinium Salts 作者:Zhi-Shi Ye,Ran-Ning Guo,Xian-Feng Cai,Mu-Wang Chen,Lei Shi,Yong-Gui Zhou |发布日期:2013.3.25 摘要:Asymmetric Hydrogenation: The Title Reaction Provides An Efficient And Rapid Access To Chiral 1‐ And 3‐substituted 1,2,3,4‐tetrahydroisoquinolines With Excellent Enantioselectivity (See Scheme; L=ligand). A Preliminary Mechanistic Study Indicates That The 1,2‐hydride Addition Might Be The Initial Step In The Reaction. The Method Has Been Used In The Synthesis Of Urinary Antispasmodic Drug (+)‐solifenacin