Copper-Catalyzed Direct C2-Benzylation of Indoles with Alkylarenes

The copper-catalyzed regioselective cross-dehydrogenative coupling of <i>N</i>-pyrimidylindoles with benzylic C­(sp³)–H bonds has been developed. Di-<i>tert</i>-butyl peroxide was employed as a mild oxidant, and benzaldehyde proved to be an effective additive. This reaction provides a direct and pratical route to a variety of 2-benzylindoles