Resolution of 1-(4-amino-3-chloro-5-cyanophenyl)-2-bromo-1-ethanol by lipase mediated enantioselective alcoholysis, hydrolysis and acylation

被引:13
作者
Conde, S
Fierros, M
Rodríguez-Franco, MI
Puig, C
机构
[1] CSIC, Inst Quim Med, E-28006 Madrid, Spain
[2] Ctr Invest, Labs ALMIRALL PRODESFARMA, Barcelona 08024, Spain
关键词
D O I
10.1016/S0957-4166(98)00252-3
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
Resolution of 1-(4-amino-3-chloro-5-cyanophenyl)-2-bromo-1-ethanol has been achieved by ethanol enantio-selective lipase-catalysed alcoholysis, hydrolysis and acylation. Although a good enantioselectivity was observed in the three reactions, the best results were obtained by hydrolysis. This alpha-bromohydrin is an intermediate in the synthesis of a new adrenergic agent. (C) 1998 Elsevier Science Ltd. All rights reserved.
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页码:2229 / 2232
页数:4
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