Demonstrates a new method to create thiazoline and thiazole macrocycles from linear peptides, suggesting broader applications in peptide synthesis.
We report a sequence-independent, chemoselective C-terminal activation platform to synthesize thiazoline/thiazole macrocycles from native linear peptides. Selective C-terminal primary amide-to-nitrile conversion proceeds in solution on fully unprotected peptides with broad functional-group compatibility. This approach eliminates the need for presynthesized α-amino nitrile building blocks and minimizes epimerization risk. Our method enables rapid macrocyclization, supporting the direct total syntheses of Mollamide F, Sanguinamide A, and Haligramide A from linear precursors.
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Le et al. (2026) studied this question.
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