Synthesis of 6-Piperazinyl-3,4-dihydroquinazolin-2(1H)-ones

A series of new 6,piperazinyl-3,4-dihydroquinazolin-2(1H)-ones have been synthesized. The described,compounds are structurally related to adoprazine, a potential atypical antipsychotics beating potent D-2 receptor antagonist and 5-HT1A receptor agonist properties Buchwald-Hartwig coupling of suitably modified aryl bromides with tert-butyl piperazinie-1-carboxylate afforded the advanced intermediate piperazinyl-3,4-dihydroquinazolin 2(1H)-one. The feductive amination of the latter With appropriately designed biarylaldehydes accomplished the synthesis of 6-piperazinyl-3,4-dihydroquinazolin-2(1H)-ones.