Synthesis and biological activity of N-substituted 2, 3, 4, 5-tetrahydro-1H-1, 5-Benzodiazepin-2-ones

BA Puodzhyunaite, RA Yanchene, ZA Talaikite…

Index: Puodzhyunaite, B. A.; Yanchene, R. A.; Talaikite, Z. A.; Zaks, A. S.; Rabotnikov, Yu. M.; Usachev, E. A. Pharmaceutical Chemistry Journal, 1985 , vol. 19, # 10 p. 686 - 690 Khimiko-Farmatsevticheskii Zhurnal, 1985 , vol. 19, # 10 p. 1195 - 1198

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Abstract

Compounds I [6], II, and III [8] were used as starting materials for the synthesis, Compound II was synthesized for the first time by fusing an equimolar mixture of o-phenylenediamine and methacrylic acid. The 5-N-acyl derivatives IV-VI were obtained by the reaction of the corresponding amines I-III with Ac20 or (EtCO) 20. The 5-N-formyl derivatives VIII and IX were obtained in yields of less than 30% from the reaction of I or II with HCOOH in dry ...