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.