A short and convenient chemoenzymatic synthesis of both enantiomers of 3-phenylGABA and 3-(4-chlorophenyl)GABA (Baclofen)

被引：60

作者：

Felluga, F ^{[1
]}

Gombac, V ^{[1
]}

Pitacco, G ^{[1
]}

Valentin, E ^{[1
]}

机构：

[1] Univ Trieste, Dipartimento Sci Chim, I-34127 Trieste, Italy

来源：

TETRAHEDRON-ASYMMETRY | 2005年 / 16卷 / 07期

关键词：

D O I：

10.1016/j.tetasy.2005.02.019

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

Both enantiomers of the pharmacologically active GABA analogues 4-amino-3-phenyl and 4-amino-3-(4-chlorophenyl)butyric acid (Baclofen) with high enantiomeric excesses were synthesized by a chemoenzymatic method involving a-chymotrypsin mediated kinetic resolutions of the corresponding 3-phenyl- and 3-(4-chlorophenyl)-4-nitrobutyric acid methyl ester precursors. (c) 2005 Elsevier Ltd. All rights reserved.

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页码：1341 / 1345

页数：5

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