Synthesis of 7,8-dichloro-6-nitro-1H-1,5-benzodiazepine-2,4-(3H, 5H) dioneas a potential NMDA receptor glycine site antagonist

Authors
Hwang, KJ
Citation
Kj. Hwang, Synthesis of 7,8-dichloro-6-nitro-1H-1,5-benzodiazepine-2,4-(3H, 5H) dioneas a potential NMDA receptor glycine site antagonist, ARCH PH RES, 23(1), 2000, pp. 31-34
Citations number
19
Categorie Soggetti
Pharmacology & Toxicology
Journal title
ARCHIVES OF PHARMACAL RESEARCH
ISSN journal
02536269 → ACNP
Volume
23
Issue
1
Year of publication
2000
Pages
31 - 34
Database
ISI
SICI code
0253-6269(200002)23:1<31:SO75D>2.0.ZU;2-L
Abstract
An efficient procedure for the preparation of 7,8-dichloro-6-nitro-1 H-1,5- benzodiazepine-2,4-(3H, 5H)-dione(7) as a potential lead compound for the N MDA receptor glycine binding site antagonist, starting from readily availab le 4,5-dichloro-2-nitroaniline(8), is described. The key step in the synthe sis involves the cyclization of malonic ester amide 10 to compound 11.