Synthesis of 2-Arylindoles by Rhodium-Catalyzed/Copper-Mediated Annulative Coupling of N-Aryl-2-aminopyridines and Propargyl Alcohols via Selective C-H/C-C Activation.

A versatile rhodium-catalyzed/copper-mediated C-H/C-C activation and cascade annulation reaction was described to form 2-arylindole derivatives. Highly selective C-C bond cleavage of γ-substituted tert-propargyl alcohols occurred, together with pyridine-directed ortho C(sp2)-H bond activation, affording a series of 2-arylindoles with yields up to 90%. Subsequent derivations were smoothly conducted to access polyfunctionalized 2-arylindoles, illustrating the potential applications of this method.