Rapid and Green Anion-Assisted Mechanochemical Peptide Cyclization

Mirko Duvnjak, Nikolina Vidović, Krunoslav Užarević, Gordan Horvat, Vladislav Tomišić, Giovanna Speranza and Nikola Cindro

A novel mechanochemical approach is described for chloride-templated head-to-tail macrocyclization of a pentapeptide and a hexapeptide. This straightforward method allows the solvent-free preparation of cyclopeptides with yields comparable to solution-based approaches without the need for high dilution of the reaction mixture and with significantly reduced reaction times and organic waste amount.

https://doi.org/10.1021/acssuschemeng.4c03309

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