SYNTHESIS OF CIS-4-AMIDO AND TRANS-4-AMIDO 2-CARBOXYTETRAHYDROQUINOLINES, HIGH-AFFINITY LIGANDS AT THE GLYCINE SITE OF THE NMDA RECEPTOR

被引：17

作者：

STEVENSON, GI

LEESON, PD

ROWLEY, M

SANDERSON, I

STANSFIELD, I

机构：

[1] Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex CM20 2QR, Terlings Park

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(00)80148-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

N-Arylimino esters (3) react with enamides (4) under Lewis acid catalysis to afford cis 4-amido-2-carboxytetrahydroquinolines (5). The products of this reaction are easily converted to the biologically active trans conformers. introduction of substituents at C-3 has no effect on affinity at the Glycine site of the NMDA receptor.

引用

页码：371 / 374

页数：4