Katritzky Salts for the Synthesis of Unnatural Amino Acids and Late-Stage Functionalization of Peptides

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.