Rhodium(III)-Catalyzed Oxidative Annulation of 7-Azaindoles and Alkynes via Double C-H Activation

Rhodium(III)-catalyzed double C-H activation involving N-directed ortho C-H activation and subsequent roll-over C-H activation of the heterocycle ring has been developed to form complex 7-azaindole derivatives in moderate to excellent yields. A broad scope of 7-azaindoles and internal alkynes has been demonstrated in this oxidative annulation reaction.