Synthesis of the HIV-Proteinase Inhibitor Saquinavir: A Challenge for Process Research

Authors

  • Wolfgang Göhring
  • Surendra Gokbale
  • Hans Hilpert Pharmaceutical Division Process Research, F. Hoffmann-La Roche Ltd., CH-4070 Basel
  • Felix Roessler
  • Markus Schlageter
  • Peter Vogt

DOI:

https://doi.org/10.2533/chimia.1996.532

Abstract

The task of process research, namely developing efficient, economically and technically as well as ecologically feasible syntheses in time, is demonstrated on the HIV-proteinase inhibitor Saquinavir, a complex molecule comprising six stereo-centres. Based on the first 26-step research synthesis furnishing a 10% overall yield, process research established a new, short 11-step synthesis affording a 50% overall yield.

Downloads

Published

1996-11-27