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

Abstract 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.