Quinazoline-Assisted Acylation with Aldehydes through Pd(II)-Catalyzed C(sp²)–H Activation

An efficient quinazoline-assisted ortho-aroylation of 4-phenylquinazolines with aromatic aldehydes has been developed using Pd(OAc)₂ as the catalyst in presence of tert-butyl hydroperoxide (TBHP). This work provides an efficient strategy to synthesis of arylketones, giving yields of up to 90%. Meanwhile, the reaction system exhibits good functional group tolerance and a wide substrate scope. Radical trapping and control experiments suggest that the aroylation reaction involves a benzoyl radical pathway.