Synthesis of 7,8-dichloro-6-nitro-1H-1,5-benzodiazepine-2,4-(3H, 5H)-dione as a potential NMDA receptor glycine site antagonist.
An efficient procedure for the preparation of 7,8-dichloro-6-nitro-1H-1,5-benzodiazepine-2,4-(3H, 5H)-dione(7) as a potential lead compound for the NMDA receptor glycine binding site antagonist, starting from readily available 4,5-dichloro-2-nitroaniline(8), is described. The key step in the synthesis involves the cyclization of malonic ester amide 10 to compound 11.
Hwang
K J
KJ
Department of Chemistry, College of Natural Science, Chonbuk National University, Chonju, Korea. Kijun@moak.chonbuk.ac.kr
D001552:Benzazepines / Q000138:chemical synthesis*; D018691:Excitatory Amino Acid Antagonists / Q000138:chemical synthesis*; D005998:Glycine / Q000378:metabolism*; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*
C407943:7,8-dichloro-6-nitro-1H-1,5-benzodiazepine-2,4-(3H,5H)-dione; D001552:Benzazepines; D018691:Excitatory Amino Acid Antagonists; D016194:Receptors, N-Methyl-D-Aspartate; D005998:Glycine