Peptide Diversification through Addition Reaction of Free Carboxylic Acids to Ynamides

Peptide modification has emerged as an important topic in the academic community and pharmaceutical industry. However, they are primarily focused on diversification of amines, thiols, alcohols. Direct chemoselective acid residues peptides is relatively underdeveloped. In this context, we report a novel efficient method for direct functionalization peptides. By using ynamides reaction partners, adducts rapidly obtained moderate to excellent yields at room temperature water. This approach shows chemoselectivity broad scope including dipeptides bearing unprotected Trp or Tyr residue free Ser Gln residue.