What is the Oseltamivir Intermidates?

Oseltamivir intermidates  was discovered at Gilead Sciences and patented in 1995. In 1996, a contract with F. Hoffmann-La Roche Ltd. was signed for the codevelopment of the drug and, after only two and a half years, a New Drug Application was filed in the United States. The drug was commercially launched in November of 1999 as the phosphoric acid salt. The discovery of oseltamivir came as the result of a search for a less polar molecule than DANA or zanamivir to prepare anorally active drug. This was accomplished by replacing the highly polar glycerol side chain by a less polar group such as 3-pentanol. In addition, it was found that the position of the double bond was critical for the potency of the drug.

The highly water-soluble phosphate salt, with a serum halflife of about 3h, is an ethyl ester prodrug that is hydrolyzed in the liver by hepatic esterases to the active form oseltamivir carboxylate.   The drug is administered orally at a dose of 75 mg twice a day. The evaluation of oseltamivir in the treatment of influenza13c as well as the synthetic approaches have been previously reviewe dinanumber of publications.