Quinazoline‐Assisted ortho‐Halogenation with N‐Halosuccinimides through Pd(II)‐Catalyzed C(sp²)−H Activation

Abstract

An efficient quinazoline-assisted ortho-halogenation of 2-arylquinazolines has been developed using N-halosuccinimides as halogen sources with Pd(II)-catalyzed CÀ H bond activation. No additional ligand and oxidant are required. This protocol is highly regioselective and applicable to a broad range of quinazoline substrates bearing different functional groups, giving yields of up to 98 %. The mechanism of the quinazoline ortho-halogenation was investigated by comprehensive experimentation.