An Efficient Conversion of the Carboxylic Group of N-Fmoc α-Amino Acids/Peptide Acids into N-Formamides Employing Isocyanates as Key Intermediates

摘要

Reaction of 96% formic acid with isocyanates derived from N-Fmoc α-amino acids/peptide acids catalyzed by DMAP has yielded a new class of stable formamides as crystalline solids which have been characterized by IR, ~1H NMR, ~(13)C NMR, and mass spectroscopy. Conversion of the side chain carboxylic acid of N-Fmoc-5-oxazolidinones of Asp/Glu into the N-formyl group also has been accomplished. The reaction is simple, mild, and high yielding.