Scientists from the Department of Chemistry at the Faculty of Science, Mirko Duvnjak, Gordan Horvat, Vladislav Tomišić, and Nikola Cindro, in collaboration with Krunoslav Užarević from the Ruđer Bošković Institute, as well as Nikolina Vidović from the Faculty of Biotechnology and Drug Development at the University of Rijeka and Giovanna Speranza from the Università degli Studi di Milano, have published a scientific paper titled Rapid and Green Anion-Assisted Mechanochemical Peptide Cyclization, in the prestigious journal ACS Sustainable Chemistry & Engineering (IF 7.1).
The paper describes a new method for preparing smaller cyclic peptides. The study reports, for the first time, the conversion of a linear peptide into a cyclic one using mechanochemistry without the presence of solvents. Traditional "head-to-tail" methods of peptide cyclization typically rely on high dilution combined with a template. This approach directs the reaction toward intramolecular cyclization, reducing unwanted intermolecular reactions of the starting compound. Such conditions require large amounts of harmful solvents like DMF, take a long time, and later necessitate solvent removal. This paper demonstrates that linear penta- and hexapeptides can be converted into cyclic peptides by grinding them with a quaternary ammonium salt and then adding the DEPBT reagent. The reaction yields are comparable to those obtained in solution, but the process is significantly faster and does not require solvents. The research was carried out as part of the HRZZ projects: NPOO.C3.2.R2-I1.06.0043, IP-2020-02-4702, and IP-2019-04-9560.
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