Palladium-catalyzed three-component carbonylative synthesis of 2-(trifluoromethyl)quinazolin-4(3H)-ones from trifluoroacetimidoyl chlorides and amines

A palladium-catalyzed three-component carbonylative reaction of trifluoroacetimidoyl chlorides and amines for the synthesis of valuable 2-(trifluoromethyl)quinazolin-4(3H)-ones has been developed. Broad substrate scope (41 examples), high efficiency (up to 99% yield) and no manipulation of CO gas constitute the notable features of this reaction. The present strategy can be applied to the late-stage modification of natural molecules and to the synthesis of the bioactive alkaloid molecule rutaecarpine.