Direct Difunctionalization of Unsaturated Peptides: A Strategy for Concurrent Incorporation of Trifluoromethyl and Alkynyl Groups

The simultaneous incorporation of alkyne and trifluoromethyl groups into peptides enables rapid access to multifunctional peptide structures. Herein, we report the first metal-free trifluoromethylalkynylation of unsaturated amino acids and peptides using a cheap trifluoromethylation reagent under mild conditions, offering a practical and versatile route to valuable scaffolds.