Technologies

This technology provides a short synthesis of Tamiflu that would be amenable to producing this important antiviral agent on a commercial scale.
Description
The technology relates to a process for the manufacture of novel intermediate useful for the preparation of Oseltamivir, and Oseltamivir Phosphate (Tamiflu) from readily available precursors and processes to prepare Oseltamivir and Oseltamivir Phosphate.
Background
World Health Organizations officials have recently warned that the risk of a human influenza pandemic remains real and is probably growing as the bird flu virus becomes entrenched in poultry in more countries. [1] The current estimated market size for Tamiflu is in excess of $2.2 billion. [2] By full-year 2007, Roche was on target to produce 400 million doses of Tamiflu.
The key market opportunity stems from the fact that there is much concern over an impending global outbreak of avian influenza. The highly pathogenic Influenza A virus subtype H5N1 virus is an emerging avian influenza virus that has been causing global concern as a potential pandemic threat. There is widespread doubt that manufacturers can supply enough doses of key antiviral medication (in particular, Tamiflu). The combination of a threat of a global-level infection, along with a compromised supply of required medication and a complex manufacturing process, creates an opportunity for a cheaper, faster and better manufacturing process
The key problem that the proposed technology overcomes is that in the current manufacturing process, shikimic acid is used in the manufacturing of Tamiflu. Shikimic acid is expensive and in limited supply, since it is obtained almost exclusively from the pods of the star anise, a fruit that is found mainly in China and whose availability has dwindled due to high demand for the flu drug. Thus, process to avoid the use of shikimic acid, and reduce the overall complexity of the manufacturing process will have commercial potential.