Discovery of KOH/BrCH2SO2F as Water‐Removable System for Clean, Mild and Robust Synthesis of Amides and Peptides

Abstract Herein we described an efficient, practical, and robust protocol for amides and peptides synthesis from carboxylic acids and amines using the combination of bromomethanesulfonyl fluoride (BMSF) with inorganic base KOH as a water‐removable system. This method is featured with broad substrate scope, excellent functional group compatibility, high yields, operational simplicity, and easy purification, which will exert great potential in amide and peptide synthesis.