Potential GABAB receptor antagonists .9. The synthesis of 3-amino-3-(4-chlorophenyl)propanoic acid, 2-amino-2-(4-chlorophenyl)ethylphosphonic acid and 2-amino-2-(4-chlorophenyl)ethanesulfonic acid

被引：12

作者：

Abbenante, G ^{[1
]}

Hughes, R ^{[1
]}

Prager, RH ^{[1
]}

机构：

[1] FLINDERS UNIV S AUSTRALIA,DEPT CHEM,ADELAIDE,SA 5001,AUSTRALIA

来源：

AUSTRALIAN JOURNAL OF CHEMISTRY | 1997年 / 50卷 / 06期

关键词：

D O I：

10.1071/C96216

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

This paper describes the synthesis of 3-amino-3-(4-chlorophenyl)propanoic acid and the corresponding phosphonic and sulfonic acids, lower homologues of baclofen, phaclofen and saclofen respectively. The chlorinated acids were all weak specific antagonists of GABA at the GABAB receptor, with the sulfonic acid (pA(2) 4.0) being stronger than the phosphonic acid (pA(2) 3.8) and carboxylic acid (pA(2) 3.5).

引用

页码：523 / 527

页数：5

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