The Mechanism of the α-Ketoacid–Hydroxylamine Amide-Forming Ligation


  • This work was supported by the Swiss National Science Foundation (200021_131957).


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Three-ring circus! Surprisingly complex molecular acrobatics are observed in the mechanism of the α-ketoacid–hydroxylamine amide-forming ligation reaction. Although this remarkable reaction can already be used for the chemoselective union of large, unprotected peptide fragments the elucidated mechanism provides important clues to extending its application to larger and more complex biological targets.