A concise and flexible synthesis of the potent anti-influenza agents tamiflu and tamiphosphor.

We report safer and more commercially viable synthetic methods for both antiinfluenza 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. All reactions are handled without using potentially hazardous intermediates or toxic reagents, and as most of the reactions occurred in a regioand stereoselective fashion to give crystalline products throughout the synthesis, the isolation procedures were relatively simple and cost effective.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.

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