The Synthesis of Phosphinic Acid Based Proteinase Inhibitors

Abstract

The phenyl phosphinate analogues of valine and phenylalanine with extended chains at phosphorus have been prepared as racemic mixtures and also in high optical purity. Kinetic data clearly indicate specific inhibitory activity for analogues having (R) configuration at α-carbon. A similar synthetic approach provides a simplified route to reported C2 symmetrical HIV inhibitors.