Fe(II)-Catalyzed Amination of Aromatic C-H Bonds via Ring Opening of 2H-Azirines: Synthesis of 213-Disubstituted Indoles

A general method for the synthesis of 2,3-disubstituted indoles is described. The key feature of this method is the amination of aromatic C-H bonds via FeCl2-catalyzed ring opening of 2H-azirines. The method tolerates a variety of functional groups such as Br, F, NO2, OMe, CF3, OTBS, alkenes, and OPiv. The method can also be extended to synthesize azaindoles.