POTENTIAL GABA-B 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

Authors
ABBENANTE G HUGHES R PRAGER RH
Citation
G. Abbenante et al., POTENTIAL GABA-B 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, Australian Journal of Chemistry, 50(6), 1997, pp. 523-527
Citations number
24
Categorie Soggetti
Chemistry
Journal title
Australian Journal of Chemistry → ACNP
ISSN journal
00049425
Volume
50
Issue
6
Year of publication
1997
Pages
523 - 527
Database
ISI
SICI code
0004-9425(1997)50:6<523:PGRA.T>2.0.ZU;2-Z
Abstract
This paper describes the synthesis of 3-amino-3-(4-chlorophenyl)propan oic acid and the corresponding phosphonic and sulfonic acids, lower ho mologues of baclofen, phaclofen and saclofen respectively. The chlorin ated acids were all weak specific antagonists of GABA at the GABAB rec eptor, with the sulfonic acid (pA(2) 4.0) being stronger than the phos phonic acid (pA(2) 3.8) and carboxylic acid (pA(2) 3.5).