Process for the preparation of a fluorolacton derivative

Patent metadata

Field	Value
Publication number	US-9845299-B2
Application number	US-201715454561-A
Country	US
Kind code	B2
Filing date	Mar 9, 2017
Priority date	Jan 14, 2013
Publication date	Dec 19, 2017
Grant date	Dec 19, 2017

Abstract

A novel process for the preparation of a fluorolactone derivative of the formula

and of its acylated derivative of formula

wherein R 1 stands for a hydroxy protecting group is described.

The acylated fluor lactones of formula V, particularly the benzoyl derivative with R 1 =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.

First claim

The invention claimed is:

1. Fluoropropionate derivative of formula

wherein A is

and wherein Ph stands for phenyl.

Assignees

• Gilead Pharmasset Llc

Inventors

• Chen Rongmin
• Li Yuanqiang
• Zhao Jianqiang
• Zheng Jianbing
• Zhu Guoliang

Classifications

• C07D307/33 Primary

  in position 2, the oxygen atom being in its keto or unsubstituted enol form · CPC title

• C07D413/06

  linked by a carbon chain containing only aliphatic carbon atoms · CPC title

• Y02P20/55

  Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups · CPC title

• C07D263/26 Primary

  with hetero atoms or acyl radicals directly attached to the ring nitrogen atom · CPC title

• A61P31/14

  for RNA viruses · CPC title