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

Org Biomol Chem. 2025 Jan 7. doi: 10.1039/d4ob01989j. Online ahead of print.

Abstract

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.