Synthesis and pharmacological activity of 1,4-benzodiazepine derivatives

摘要

3,4-Dihydro-1H-benzo[3][1,4]diazepine-2,5-dione 1 has been prepared from the reaction of glycine with isatoic anhydride. Bromination of 1 with molecular bromine in acetic acid affords the 7-bromo derivative 2. Paartial and full reduction of 2 with Li-AlH_4 gives the 7-bromo-1,2,3,4-tetrahydrobenzo[3][1,4]diaze-pine 4, respectively. The reaction of 3 with alkyl and acyl halides produces the corresponding derivatives 5. Preliminary pharmacol-ogical screening of some of the newly synthesized compounds reveal that they exhibit CNS-depressang and anticonvulsant activity.