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 α-amino acids and peptides is of great importance for biochemical study and pharmaceutical development. Few methods based on remote C(sp³)-H functionalization of aliphatic side-chains of peptides has been disclosed in recent years. In this report, we developed a novel approach for γ-C(sp³)-H and γ-/δ-C(sp²)-H arylation of α-amino acids with α-hydrogen by native amine-directed C-H functionalization and further realized the γ-C(sp³)-H arylation of N-terminally unprotected peptides.