2-(1-(4-(N-phenyl-N-propionyl)amino)piperidyl)-hexahydro- 1H-1,4- diazepine 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 1^H NMR. Compounds of 9a～9d and 10a～10d were tested for their biological activities.

Key words: ARYL GROUP, ETHANE P, ACETAMIDE P, OPIUM, ACCEPTOR, KINETIN, SYNTHESIS METHODS