Gilead Pharmasset LLC

Lonza Ag

Lonza Guangzhou Research & Development Center Ltd

Rongmin Chen

Guoliang Zhu

Yuanqiang Li

Jianqiang Zhao

Jianbing Zheng

Wilhelm Quittmann

Feng Ye

Wei Zhu

A novel process for the preparation of a fluorolactone derivative of the formula   The acylated fluor lactones of formula V, particularly the benzoyl derivative with R=benzyl are important precursors for the synthesis of prodrug compounds which have the potential to be potent inhibitors of the Hepatitis C Virus (HCV) NS5B polymerase.

Process for the preparation of a fluorolacton derivative

A novel process for the preparation of a fluorolactone derivative of the formula   The acylated fluorolactones of formula V, particularly the benzoyl derivative with R=benzyl are important precursors for the synthesis of prodrug compounds which have the potential to be potent inhibitors of the Hepatitis C Virus (HCV) NS5B polymerase.

Method of synthesizing a compound of formula (I), wherein R1, R2 are, independently, chloro or fluoro, and wherein R3 is H, alkyl, aralkyl or is an alkylether or alkylthioether comprising the steps of firstly reducing a diazeny compound of formula (II) non-catalytically or with a catalytic amount of an homogenous organic, non-metal catalyst to the corresponding hydrazo compound of formula (III) and in a second step catalytically hydrogenating said hydrazo compound in with a heterogeneous Ni-catalyst to the compound of formula (I). 

Reduction of 5-(aryl-diazenyl)-4,6-dihalo-pyrimidine

Growing community of inventors

Guangzhou, China

Rongmin Chen