Synthesis of novel quinazolinone derivatives

2, 6-Dicyanoaniline derivatives(3) were synthesized from the multi-component condensation of aldehyde, malononitrile and ketone under the catalysis of ammonium acetate. Then 2, 6-dicyanoaniline derivatives reacted with ketones to give mutli-substituted quinazolinone derivatives(5) using sodium hydroxide as catalyst at 100°C or refluxing through intermolecule Pinner reaction via Dimroth rearrangement. The structures of the synthetic compounds were characterized by IR, ¹H NMR, ¹³C NMR and MS. Quinazolinone derivatives are the important inter-mediate of a series of drugs.