Synthesis of 4-ethenyl quinazolines via rhodium(iii)-catalyzed [5 + 1] annulation reaction of N-arylamidines with cyclopropenones

Abstract

An unprecedented synthesis of 4-ethenyl quinazolines via a Rh(III)-catalyzed C–H activation and annulation reaction was described. In particular, when C-alkyl imidamides are benzyl groups, 2-benzoyl quinazolines can be obtained. This protocol enables the effective application of cyclopropenones, featuring high atom efficiency, broad substrate scope and mild reaction conditions.