A Concise and Flexible Synthesis of the Potent Anti-Influenza Agents Tamiflu and Tamiphosphor

摘要

Influenza remains a major health problem.The worldwide occurrences of avian flu have increased public awareness of the potential for global influenza pandemics.Tamiflu(oselta-mivir phosphate,1·H3PO4;Scheme 1),a popular drug for the treatment of influenza,is an orally administrated prodrug which is readily hydrolyzed by hepatic esterases to give the corresponding carboxylic acid 2 as the active inhibitor of neuraminidase on the influenza virus.As the side effects of tamiflu cause teenage patients to suffer from mental disorders,'21 and with the emergence of drug-resistant strains of avian flu,the development of new chemical entities to combat influenza viruses are urgently needed for the battle against the threat of pandemic flu.