Efficient Synthesis of C–N-Coupled Heterobiaryls by Sequential N–H Functionalization Reactions

C–N-coupled heterobiaryls were synthesized by sequential N–H functionalization reactions: stereoselective rhodium-catalyzed N–H insertion, followed by regioselective palladium-catalyzed C–H amination. Because of the good substrate scope and excellent selectivity, the developed method presents a novel approach for the synthesis of heterobiaryls, which are potent antibiotics.