The Nickel/Copper-Catalyzed Direct Alkylation of Heterocyclic C-H Bonds

A general and straightforward protocol for the cross-coupling of non-activated alkyl halides with heterocyclic CH bonds has been developed. The transformation is chemo- and regioselective and many functional groups on both coupling partners are tolerated. The method employs cheap nickel/copper catalysts, and expands significantly the scope of CH functionalization.