Direct, Chemoselective N‐tert‐Prenylation of Indoles by CH Functionalization

Abstract

Four steps in one: The direct prenylation of indoles at N-1 can be achieved by CH functionalization in the presence of a PdII source. This reaction proceeds by direct intermolecular olefin amination, tolerates a broad range of functional groups, and can be carried out on a gram scale, as demonstrated by the formal syntheses of a number of natural products and the synthesis of an antifungal natural product (see scheme).