Synthesis of retro-inverso peptides employing isocyanates of N~(alpha)-Fmoc-amino acids/peptide acids catalyzed by DMAP

摘要

The Goldschmidt-Wick type reaction between isocyanates of N~(alpha)-Fmoc-amino acids/peptide acids and N~(alpha)-Boc-/Z-/ Bsmoc-amino acids catalyzed by DMAP leads to the incorporation of a reversed peptide bond.It was found to be a simple,efficient and clean reaction.All the retro-inverso peptides made were obtained as crystalline compounds in 70-92% yields.