Regio- and enantioselective synthesis of N-allylindoles by iridium-catalyzed allylic amination/transition-metal-catalyzed cyclization reactions.

Regio- and enantioselective synthesis of N-allylindoles was realized through an iridium-catalyzed asymmetric allylic amination reaction with 2-alkynylanilines and subsequent transition-metal-catalyzed cyclization reactions. The highly enantioenriched allylic amines prepared from Ir-catalysis were treated with catalytic amount of NaAuCl4⋅2 H2O or PdCl2 providing various substituted N-allylindoles in excellent yields and enantioselectivities.