Site‐Selective Trifluoromethylation Reactions of Oligopeptides

Site‐selective chemical modifications that target proteinogenic amino acid residues complement the methods entailing genetic manipulation, thereby allowing straightforward and rapid access to engineered proteins. The incorporation of the trifluoromethyl group into amino acids within a peptide sequence results in relevant peptidomimetics with unique biomedicinal properties. As a result, the last decade has witnessed the development of a powerful set of protocols toward the selective trifluoromethylation of small‐to‐medium size peptides and proteins in a late‐stage fashion. This minireview seeks to highlight those particularly compelling cases published in the last years.