Synthesis of 2,3-Disubstituted NH Indoles via Rhodium(III)-Catalyzed C–H Activation of Arylnitrones and Coupling with Diazo Compounds

A rhodium-catalyzed intermolecular coupling between arylnitrones and diazo compounds by C–H activation/[4 + 1] annulation with a C­(N2)–C­(acyl) bond cleavage is reported, and 2,3-disubstituted NH indoles are directly synthesized in up to a 94% yield. A variety of functional groups are applicable to this reaction to give the corresponding products with high selectivity. Compared to other previously reported Rh­(III)-catalyzed synthesis of homologous series, this method is simpler, more general, and more efficient.