Rhodium-catalyzed regioselective ortho-allylation of 2,4-diarylquinazolines with allylic acetate

Abstract

In this paper, a rhodium-catalyzed regioselective reaction of 2,4-diarylquinazolines with allylic acetate is described, leading to allylated quinazoline derivatives with high efficiency and good tolerance of functional groups. By switching to 2-arylquinazolin-4-ones, tandem C–H activation and aza-Michael addition are involved, leading to 1,6-dimethyl-5H-isoquinolino[1,2-b]quinazolin-8(6H)-one derivatives with high efficiency.