Fig. 1. Peptide macrocyclization strategies and functionalization of the β-carbon of amino acids at the N-terminus of peptides via site-selective C(sp3)–H activation. (a) Current peptide macrocyclization strategies. (b) Intermolecular arylation of peptides at the N-terminus via C(sp3)–H activation. (c) Intramolecular macrocyclization of peptides via C(sp3)–H activation. Phth = phthaloyl.
