Add time:07/12/2019         Source:sciencedirect.com

α-Substituted amines are present in a myriad of biologically active natural and synthetic products. With the objective of developing atom-economical reactions, a panel of synthetic methods allowing the direct functionalization of C(sp3)‒H bonds adjacent to the nitrogen atom have been developed. The field remains dominated by the sequence α-lithiation/addition on an electrophile even if the use of reactive organolithium reagents is not compatible with all functional groups. Over the past ten years, an increasing interest has been devoted to metal-catalyzed CH-activation, some studies being specially dedicated to C(sp3)‒H bond activation. Notably, this approach has been envisioned to perform direct α-functionalization of amines. The aim of this article is to give an overview of synthetic methods for transition metal-catalyzed α-alkylation of amines by C(sp3)‒H bond activation.

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