Rhodium-Catalyzed Regioselective C7-Functionalization of Indole Derivatives with Acrylates by Using an N-Imino Directing GroupWe are grateful to the Shanghai Sailing Program (17YF1418900) and Merck for their financial support.
Received: 07 June 2017
Accepted after revision: 06 July 2017
17 August 2017 (eFirst)
Dedicated to Professor Victor Snieckus on the occasion of his 80th birthday
An efficient rhodium-catalyzed method for C–H olefination at the C7 position of indoles has been developed. The N-imino directing group was shown to be crucial for high regioselectivity and reactivity of the metal catalyst. The utility of this protocol was further demonstrated through a concise, four-step synthesis of pyroquilon from indole.