6-PIPERAZINYL-3,4-DIHYDROQUINAZOLIN-2(1H)-ONES

摘要

A series of new 6-piperazinyl-3,4-dihydroquinazolin-2(1H)-ones have been synthesized. The compounds are structurally related to adoprazine, a potential atypical antipsychotics bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties. Buchwald-Hartwig coupling of suitably modified aryl bromides with tert-butyl piperazine-1-carboxylate afforded the advanced intermediate piperazinyl-3,4-dihydroquinazolin-2(1H)-one. The reductive amination of the latter with appropriately designed biarylaldehydes accomplished the synthesis of these compounds.

主权项

1. A therapeutic agent comprising:
a dihydroquinazolinone compound of formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient wherein R is selected from the group consisting of: and a pharmaceutically acceptable excipient selected from the group consisting of carboxymethylcellulose, methyl cellulose, hydropropylmethylcellulose, sodium alginate, polyvinylpyrrolidone, gum tragacanth, gum acacia, calcium carbonate, sodium carbonate, lactose, calcium phosphate, and sodium phosphate.