Copper-Catalyzed C-2 Arylation or Vinylation of Indole Derivatives with Iodonium Salts

Copper-catalyzed C-2 arylation and vinylation of indole derivatives with iodonium salts have been realized. This method, featuring a simple operational procedure, mild reaction conditions, and a wide substrate scope, provided versatile indole derivatives with direct and selective functionalization at the C-2 position of the indole core. In the presence of excess amounts of iodonium salts, cascade C-2 arylation and dearomatization through the C-3 arylation reaction also proceeded smoothly.