Sulfonylcarbamates as Amino Protecting Groups in Peptide Chemistry

Abstract
In a search for new peptide coupling agents N-acetyl-L-phenylalanine and methyl L-alaninate were treated with p-tosylisocyanate in the hope of obtaining the model racemization peptide methyl N-acetyl-L-phenylalanyl-L-alaninate and benzenesulfonamide.1 Instead, the reaction gave in moderate yield alanyl tosylhydantoin, identified by an independent synthesis and spectral data. This result suggested that the treatment of an amino acid (1) with p-tosyliso-cyanate (2) would yield the corresponding p-tosyl-aminocarbonyl derivative (3) or Tac-Amino acid.

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