Carbonylation of α-Aminoalkyl radicals to the direct synthesis of α-Amino acid derivatives

Abstract

α-Amino acid derivatives are indispensable motifs in various areas. Herein, we developed an unprecedented and general α-aminoalkyl carbonylation protocol that activates a variety of inert C–H bonds as native functional handles toward the direct synthesis of various α-amino acid derivatives. The key to the success of this mode is the installation of an appropriate electron-withdrawing group which can modulate the nucleophilicity of the α-aminoalkyl radical and provides a matching polarity for the subsequent carbonylation process. This catalytic strategy features a remarkably broad substrate scope and excellent tolerance of sensitive functional groups, offering general and practical access to α-amino acid derivatives.