Synthesis of an enantiomerically pure aminoisoquinocarbazole with antiarrhythmic activity via lipase-catalyzed enantioselective transesterification

被引:44
作者
Fukazawa, T [1 ]
Shimoji, Y [1 ]
Hashimoto, T [1 ]
机构
[1] SANKYO CO LTD,SANKYO RES LABS,SINAGAWA KU,TOKYO 140,JAPAN
关键词
D O I
10.1016/0957-4166(96)00199-1
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
Enantiomerically pure (R)-2-cydohexen-1-ol 5 was prepared via lipase-catalyzed enantioselective transesterification of 2-substituted cyclohexanol, and stereospecifically converted to (-)-(2-cyclohexenyl)acetic acid 4. Enantiomerically pure aminoisoquinocarbazole 1 (RS-2135) was synthesized stereoselectively from 4, using an intramolecular Dids-Alder reaction and Curtius rearrangement. Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码:1649 / 1658
页数:10
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