Js. Shen et al., Synthesis of Hexahydro-1H-1,4-diazepine analogues carrying the segment of (1-arylacetamide-2-tertiaryamide) ethane (II), ACT CHIM S, 59(8), 2001, pp. 1317-1322
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 sub
stitution, and debenzylation. Seven target compounds of hexahydro-1H-1,4-di
azepine analogues carrying the segment of (1- arylacetamide-2-tertiaryamide
) ethane were synthesized through selective acylation and acylation of comp
ound 7, and the four target compounds 10a similar to 10d containing hydroph
ilic group of hydroxy were achieved through debenzylation of 9a, 9b, 9c and
9d. These products were characterized by IR, EIMS, elementary analysis and
H-1 NMR. Compounds of 9a similar to 9g and 10a similar to 10d were tested
for their biological activities.