Biocompatible synthesis of macrocyclic thiazole peptides from chiral α-amino nitriles

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Shang, Minghao
He, Junming
Gardiner, Michael G.
Nitsche, Christoph

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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 alpha-amino nitriles enables the incorporation of diverse hydrophobic side chains adjacent to the thiazole motif.

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Organic and Biomolecular Chemistry

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