Molecular Oxygen-Mediated Radical Alkylation of C(sp3)–H Bonds with Boronic Acids

A direct and site-specific alkylation of (sp³)C-H bond with aliphatic boronic acid was achieved. By simply heating glycinates and amines together with alkylboronic acids under an oxygen atmosphere, a variety of unnatural α-amino acids and peptides could be obtained in good yields.