The synthesis of phosphinic acid based proteinase inhibitors

Article abstract of DOI:10.1080/10426509908546356

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.