Synthesis of Indoles through Palladium-Catalyzed Three-Component Reaction of Aryl Iodides, Alkynes, and Diaziridinone

The three-component reaction of aryl iodides, alkynes, and diaziridinone is described. The reaction provides an innovative synthetic approach for indoles. The approach features high efficiency, broad substrate scope, and excellent regioselectivity. C,C-Palladacycles should act as the intermediates. The C,C-palladacycles are obtained from simple aryl halides and alkynes and then reacted with diaziridinone to afford indoles.