Levashov D. Synthesis of 2-(diarylhydroxymethyl)-3-R-3,4-dihydro-4-oxoquinazolines, their physical and chemical properties and biological activivty..

First time the 2-(diarylhydroxymethyl)-3-R-3,4-dihydro-4-oxoquinazolines that combin in a single molecule a quinazoline heterocycle and the moiety of benzylic (diphenylhydroxyacetic) acid, two active pharmacophores was obtained. A new effective method for 2-carbethoxy-3-aryl-3,4-dihydro-4-oxoquinazolines by heterocyclizations have been proposed. New data about poorly investigated interaction of 3,4-dihydro-4-oxoquinazolines with Grignard reagents were obtained: for the first time shown that interaction between 2-carbethoxy-3-R-3,4-dihydro-4-oxoquinazolines and arylmagnesium halides is carried out with ester group only. The case of easy hydrolytic opening quinazolinone cycle for 2-R-3-furfuryl-3,4-dihydro-4-oxoquinazolines has been described. For the first time under the heterocyclizations of N-ethoxalylanthranilic acid benzylamide a benzodiazepine derivative – 2-carbethoxy-3-phenyl-5-oxo-1,4-benzodiazepine was obtained. Among the synthesized 2-(diarylhydroxymethyl)-3-R-3,4-dihydro-4-oxoquinazolines compounds showing a significant level of anticonvulsant activity were found