Sequential one-pot Rh(III)-catalyzed direct C2 and C7 alkylation of (hetero)aromatic C-H bonds of indoles

A simple and versatile method for the highly efficient synthesis of a series of disubstituted indoles via a sequential one-pot Rh(III)-catalyzed direct C2-H and C7-H alkylation with diazo compounds has been developed. This process features with mild reaction conditions, wide substrate scope, and good functional group tolerance (24 examples, up to 96% yield).