ИСТИНА

This report presents the results of the development of the N+PC methodology for the synthesis of phosphinic pseudo-tripeptides by amidoalkylation of phosphonous carboxylic acids followed by peptide synthesis. This original approach is based on the results of the mechanism investigation of the phosphorus-carbon bond formation in the reaction under study. We found that the lactone structural motif is preserved during all transformations starting from P(III)-phospholactone (with a three-coordinated phosphorus atom) to the formation of P(V)-phospholactone (spirophosphorane) and then to P(IV)-phospholactone (with a four-coordinated phosphorus) with followed formation of phosphinic dipeptide.