Enantioselective syntheses of (-)-(R)-rolipram, (-)-(R)-baclofen and other GABA analogues via rhodium-catalyzed conjugate addition of arylboronic acids

被引：48

作者：

Becht, JM ^{[1
]}

Meyer, O ^{[1
]}

Helmchen, G ^{[1
]}

机构：

[1] Heidelberg Univ, Inst Organ Chem, D-69120 Heidelberg, Germany

来源：

SYNTHESIS-STUTTGART | 2003年 / 18期

关键词：

asymmetric synthesis; catalysis; conjugate addition; rhodium; arylboronic acid;

D O I：

10.1055/s-2003-42457

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Highly enantioselective syntheses of two important gamma-aminobutyric acid (GABA) analogues, the antispastic drug (-)-(R)-Baclofen and the antidepressant agent (-)-(R)-Rolipram, are reported. Key-steps in both syntheses are the Rh-catalyzed asymmetric of arylboronic acids to 4-aminobut-2,3-enoic acid derivatives.

引用

页码：2805 / 2810

页数：6

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