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
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
收藏
页码:371 / 374
页数:4
相关论文
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