Efficient Protocol for the Synthesis of N‐Phosphorodiamidate Peptidomimetics

Abstract Phosphoryl peptidomimetics represent a novel class of peptide analogs that have garnered attention due to their unique synthetic pathways. Employing a combination of Tf 2 O and pyridine, the amino acid phosphoryl diester transforms into a phosphorodiamidate compound. This conversion involves activating one of the ester moieties, yielding a good product. This protocol is characterized by its straightforward and comprehensive approach, making it a notable advancement in the chemistry of peptidomimetics.