The Study On The Synthesis Of4-Hydroxy-1,2,3,4-Benzo[b]Azepine-5-One And1,2,3,4-Tetrahydro Benzo [b] Azepine-5-one

The2,3,4,5-tetrahydro-1H-benzo[b]azepine (1-benzazepine) scaffold has promising biological activities toward various targets such as enzymes,12-16ion channels,1and G-proteincoupled receptors (GPCRs)We study on the synthesis process of4-hydroxy-1,2,3,4-tetrahydro benzo [b] azepine-5-one and1,2,3,4-Tetrahydro-benzo [b] azepine-5-one which have been reported.We Optimise the synthesis process of4-hydroxy-1,2,3,4-tetrahydro benzo [b] azepine-5-oneDepended on the structure of1,2,3,4-tetrahydro benzo [b] azepine-5-one, we developed a new synthetic route in order to get a higher yield and good industrial value. The raw material is aniline, aniline is substituted by4-bromo-, ethyl butyrate, and then amine is protected, and then saponification, acidification, and finally the F-C acylation, deprotection. We select cbz as protecting groups for amine. Finally We found using cbz as protecting groups F-C cyclization, the yield is21%and tatal yield is12.8%for he entire route. For the process route of1,2,3,4-Tetrahydro-benzo [b] azepine-5-one, the yield and cost does not have any advantage. But for latter study of the1,2,3,4-Tetrahydro-benzo [b] azepine-5-one, we provide a certain foundation.