image adapted from https://next.cancer.gov/discoveryResources/cbc.htm, Division of Cancer Treatment and Diagnosis, National Cancer Institute, part of the U.S. National Institutes of Health’
IRBM review article on Katritzky salts (as intermediates for the synthesis of unnatural amino acids, late-stage functionalization of peptides, and macrocyclization) is featured on the cover of the European Journal of Organic Chemistry
Innovative synthetic strategies giving access to a larger chemical space are of great importance to make the development of peptide therapeutics a faster and more efficient process. Katritzky salts, easily prepared from primary amines, offer peptide chemists a tool to achieve many chemical transformations in a straightforward manner. The IRBM peptide chemistry group is proud to share the publication of a review article in the European Journal of Organic Chemistry covering the application of Katritzky salts in the synthesis of unnatural amino acids, in the late-stage functionalization of peptides (from smaller dipeptides to more complex biomolecules), and as an alternative methodology to allow macrocyclization of linear peptides. The review also describes a more recent application where the viability of deaminative functionalization of Katritzky salts during solid-phase peptide synthesis (SPPS), significantly expands the scope of such precursors for the effective chemical exploration of peptides and biomolecules.