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

Org Lett

§Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.

Published: June 2015

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.

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http://dx.doi.org/10.1021/acs.orglett.5b01228DOI Listing

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