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

Abstract

Abstract An economical and efficient approach to pharmaceutically and biologically significant 2,3‐dihydroquinazolin‐4(1 H )‐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. magnified image