Chemical Research in Chinese Universities ›› 2006, Vol. 22 ›› Issue (1): 51-55.

• Articles • Previous Articles     Next Articles

An Improved Synthetic Method of Saquinavir

YANG Qin-gang, HE Xu-chang, LEI Li-jun, ZHOU Qi-ting, BAI Dong-lu   

  1. Shanghai Institute of Materia Medica, Shanghai Institutes of Biological Sciences,Chinese Academy of Sciences, Shanghai 201203, P. R. China
  • Received:2005-03-01 Online:2006-02-24 Published:2011-08-06
  • Supported by:

    Supported by the Science and Technology Commission of Shanghai Municipality(No. 024319126).

Abstract: An improved synthetic method of saquinavir, an HIV protease inhibitor, is described. In comparison with the methods in the reported works, the improved procedures had several advantages, such as less expensive agents, shorter reaction time, and a smaller amount of the solvent needed. To measure the optical purities of the products, the intermediates were determined by means of chiral HPLC. Some of the intermediates can also be used for the preparation of new protease inhibitors.

Key words: HIV, Protease inhibitor, Saquinavir, Synthesis