Fe(II)-catalyzed amination of aromatic C-H bonds via ring opening of 2 H-azirines: Synthesis of 2,3-disubstituted indoles

摘要

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 FeCl_2-catalyzed ring opening of 2H-azirines. The method tolerates a variety of functional groups such as Br, F, NO_2, OMe, CF_3, OTBS, alkenes, and OPiv. The method can also be extended to synthesize azaindoles.