Site-Selective Modification of α-Amino Acids and Oligopeptides via Native Amine-Directed γ-C(sp3)-H Arylation

Site-selective modification of chemically and biologically valuable alpha-amino acids and peptides is of great importance for biochemical study and pharmaceutical development. Few methods based on remote C(sp(3))-H functionalization of aliphatic side-chains of peptides has been disclosed in recent years. In this report, we developed a novel approach for gamma-C(sp(3))-H and gamma-/delta-C(sp(2))-H arylation of alpha-amino acids with alpha-hydrogen by native amine-directed C-H functionalization and further realized the gamma-C(sp(3))-H arylation of N-terminally unprotected peptides.