Cysteine‐Free Peptide and Glycopeptide Ligation by Direct Aminolysis

Abstract

Left to their own devices in a mixed-solvent system, peptides undergo efficient aminolysis with peptide thioesters (see scheme). This ligation method, which does not require coupling reagents, auxiliaries, or an N-terminal cysteine residue, is suitable for a variety of amino acids at the ligation junction. Its effectiveness was demonstrated by the synthesis of a 6.9-kDa section of the cancer-associated MUC1 tandem repeat. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2002/2008/z705298_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.