Journal of the American Chemical Society

Palladium-catalyzed direct 2-alkylation of indoles by norbornene-mediated regioselective cascade C–H activation

L Jiao, T Bach

Index: Jiao, Lei; Bach, Thorsten Journal of the American Chemical Society, 2011 , vol. 133, # 33 p. 12990 - 12993

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Citation Number: 132

Abstract

A palladium-catalyzed direct 2-alkylation reaction of free NH indoles has been developed. This reaction relies on a norbornene-mediated cascade C–H activation process at the indole ring, which features high regioselectivity and excellent functional group tolerance. The reaction represents the first example for a generally applicable, direct C–H alkylation of indole at the 2-position.