PROCESSES FOR COUPLING AMINO ACIDS USING BIS-(TRICHLOROMETHYL) CARBONATE

摘要

A process is disclosed for using triphosgene as an efficient and effective coupling reagent during peptide synthesis, by in situ generation of amino ac id chloride from a protected amino acid. This process is particularly useful fo r the coupling to sterically hindered amino acid residues, or for other difficult couplings. Furthermore, the same reagent can be used for the derivatization of peptides by formation of an amide bond between a free amin e on a peptide and a carboxylic acid, or for the coupling of an amino acid to a solid support.