Synthesis of α-Trifluoromethyl-α-hydroxy Acid--Peptide Conjugates via Click Chemistry.

A simple and convenient method for the incorporation of fluorinated α-hydroxy acids into peptides is described. The target conjugates were obtained from α-alkynyl-α-trifluoromethyl-α-hydroxy acids and azido peptides via the copper(I)-catalyzed Huisgen cycloaddition reaction (click chemistry). After straightforward deprotection, the α-trifluoromethyl-α-hydroxy acid containing peptides may find important applications in biochemistry and medicinal chemistry. [ABSTRACT FROM AUTHOR]