Abstract

Oseltamivir phosphate (Tamiflu®) is the only orally active anti-influenza drug that potently inhibit neuraminidase. The recent emergence of avian flu, especially the H5N1 type, makes the situation of Tamiflu supply and demand increasingly serious. Further optimization of the current commercial approach and exploration of new synthetic routes are urgent. Here, different synthetic strategies of oseltamivir phosphate are reviewed, including discovery and improved synthetic route from (-)-quinic acid or (-)-shikimic acid, new asymmetric synthesis via catalytic desymmetrization of a mesoaziridine (CDMA), Diels-Alder Reaction and from other available materials.

Keywords: Oseltamivir phosphate (Tamiflu), neuraminidase inhibitor, synthetic strategies