A Novel Industrialized Synthetic Route Of Tamiflu

As an anti-influenza drugs,Tamiflu is the most effective and most specific virus neuraminidase inhibitors.So far,there are 44 synthetic routes of Tamiflu,of which 22 are natural compounds as the starting material.According to the limitation of the natural conditions,the supply of natural compounds are always unstable,therefore we develop a scale-up process of Tamiflu based on the fundamental chemicals.By employing the available intermediate 6SCH of our company,a novel synthetic process is developed.Firstly,6SCH is converted to OTVP-A by configuration transformation.After one-pot synthesis including hydrogenation,amino Boc protection and saponification,OTVP-A is then transformed into OTVP-C.OTVP-C goes through one-pot decarboxylation,acetylization and elimination method to obtain OTVP-F.Finally OTVP is provided after Boc deprotection and phosphoric acid salification of OTVP-F with total yield 55.4%.In terms of the advantages such as cheap raw materials & regents,mild & highly effective reaction conditions,easily controllable operations,good equipment compatibility,lower overall cost,the developed procedure is a very suitable manufacturing route.