Synthesis of hexahydro-1H-1,4-diazepine analogues carrying the segment of (1-arylacetamide-2-tertiaryamide) ethane (II)

2-(1-(4-(N-phenyl-N-propionyl)amino)piperidyl)-hexahydro-1H-1,4-diazepin e 7 was prepared starting from 3 through reduction, chlorination, amine substitution, and debenzylation. Seven target compounds of hexahydro-1H-1,4-diazepine analogues carrying the segment of (1-arylacetamide-2-tertiaryamide) ethane were synthesized through selective acylation and acylation of compound 7, and the four target compounds 10a-10d containing hydrophilic group of hydroxy were achieved through debenzylation of 9a, 9b, 9c and 9d. These products were characterized by IR, EIMS, elementary analysis and 1H NMR. Compounds of 9a-9g and 10a-10d were tested for their biological activities.