A Concise and Flexible Synthesis of the Potent

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A Concise and Flexible Synthesis of the Potent
Anti-Influenza Agents Tamiflu and Tamiphosphor
Jiun-Jie Shie, Jim-Min Fang, and Chi-Huey Wong
(Genomics Research Center, Academia
Sinica) Angewandte Chemie International Edition
47(2008)57885791
We report safer and more commercially viable
synthetic methods for both anti-influenza drugs
Tamiflu and Tamiphosphor using bromobenzene as
the starting material. This is an innovative
procedure in which the bromine atom is converted
to carboxyl or phosphonate groups at the later
stage. Like Tamiflu, Tamiphosphor can be taken
orally, and functions as an inhibitor of the
neuraminidase active site of the H5N1/H1N1
viruses. However, Tamiphosphor proves to be more
effective due to its higher enzyme inhibition.
Survival rates and recovery rates of infected
mice treated with Tamiphosphor both show better
results.