Stereocontrolled synthesis and biological activity of two diastereoisomers of the potent HIV-1 protease inhibitor saquinavir.

@article{Righi2008StereocontrolledSA,
  title={Stereocontrolled synthesis and biological activity of two diastereoisomers of the potent HIV-1 protease inhibitor saquinavir.},
  author={Giuliana Righi and Simona Ciambrone and Carlo Bonini and Pietro Campaner},
  journal={Bioorganic & medicinal chemistry},
  year={2008},
  volume={16 2},
  pages={902-8}
}
A general enantioselective synthesis of new syn-hydroxyethylamine isosteres has been developed. The approach, based on the controlled opening of functionalized optically active 2,3-epoxy amines, can be conveniently used for the preparation of new peptidomimetics with various residues. Finally the total synthesis of two diastereoisomer analogues of HIV-Protease inhibitor Saquinavir has been achieved and their biological activity evaluated.