The Synthetic-Technical Development of Oseltamivir Phosphate Tamiflu™: A Race against Time

Authors

  • Stefan Abrecht
  • René Trussardi
  • Gösta Rimmler
  • Thomas Oberhauser
  • Hans-Jürgen Mair
  • Martin Karpf
  • Rolf Fischer
  • Heinrich Estermann
  • Muriel Cordon Federspiel
  • Ulrich Zutter

DOI:

https://doi.org/10.2533/chimia.2007.93

Keywords:

Analytics, Influenza neuraminidase inhibitor, Oseltamivir phosphate, Production, Synthesis, Technical development

Abstract

The clinical development of the first orally available neuraminidase inhibitor prodrug oseltamivir phosphate (Tamiflu™) proceeded very fast. In order to support this program an unprecedented team effort in chemical process research, development, piloting, production and analytics took place, which allowed the successful launch of Tamiflu™ in 1999, only two and a half years after it was licensed from Gilead Sciences. This article describes selected aspects of the commercially used synthesis route and a brief summary of alternative syntheses devised by Roche chemists.

Downloads

Published

2007-03-28

Issue

Section

Scientific Articles