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

[Display omitted] • A new procedure for the synthesis of α -amino acid derivatives has been developed. • Carbonylation of α -aminoalkyl radical has been achieved. • A variety of various α-amino acid derivatives were prepared in good yields with very good substrate tolerance. 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. [ABSTRACT FROM AUTHOR]