Macrocyclic peptides containing a thiazole heterocycle exhibit fascinating properties in natural products and future therapeutics. We report a biocompatible macrocyclisation approach facilitated by an N-terminal cysteine and C-terminal nitriles. The use of various chiral α-amino nitriles enables the incorporation of diverse hydrophobic side chains adjacent to the thiazole motif.
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M. Shang, J. He, M. G. Gardiner and C. Nitsche, Org. Biomol. Chem., 2025, Advance Article , DOI: 10.1039/D4OB01989J
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