In this study, we present an efficient and direct strategy for the synthesis of N1,N3-disubstituted quinazoline-2,4(1H,3H)-diones with high atom and step economy. The protocol involves a Pd(II)-catalyzed 3 + 1 + 1 + 1 cascade carbonylation/amidation/cyclocarbonylation reaction, wherein the alkylamino moiety of simple N-substituted anilines serves as an intrinsic directing group, with CO and amines as the coupling partners. This cascade process proceeds smoothly with a variety of substrates under mild conditions, affording the target products with either identical or distinct substituents mostly in moderate to good yields.
Zhang et al. (Mon,) studied this question.