Alkylamino-Directed One-Pot Reaction of N-Alkyl Anilines with CO, Amines and Aldehydes Leading to 2,3-Dihydroquinazolin-4(1H)-ones

An economical and efficient approach to pharmaceutically and biologically significant 2,3-dihydroquinazolin-4(1H)-ones has been disclosed. The one-pot multicomponent reaction was performed through a palladium-catalyzed ortho-selective oxidative carbonylation of N-substituted anilines with CO and primary amines, and subsequent condensation with aldehydes in MeCN by using alkylamino as the directing group, KI/AcOH as the additives, and Cu(OAc)(2) as the oxidant. This intriguing straightforward method features embedded directing strategy, simple starting materials, mild conditions, high atom/step economic economy, broad substrate scope and good product diversity.