Hypervalent Iodine‐Mediated Late‐Stage Peptide and Protein Functionalization

Hypervalent iodine compounds are powerful reagents for the development of novel transformations. As they exhibit low toxicity, high functional group tolerance, and stability in biocompatible media, they have been used for the functionalization of biomolecules. Herein, we report recent advances up to June 2021 in peptide and protein modification using hypervalent iodine reagents. Their use as group transfer or oxidizing reagents is discussed in this Minireview, including methods targeting polar, aromatic, or aliphatic amino acids and peptide termini. Hypervalent iodine reagents are commonly used for the development of novel transformations. As they are highly reactive and biocompatible, they have been employed more recently for the functionalization of biomolecules. This Minireview discusses the development of hypervalent iodine reagents for the modification of peptides and proteins as well as their application, such as for labeling and peptide stapling.