Process for the preparation of a fluorolacton derivative

摘要

A novel process for the preparation of a fluorolactone derivative of the formula;and of its acylated derivative of formula;wherein R1 stands for a hydroxy protecting group is described.;The acylated fluorolactones of formula V, particularly the benzoyl derivative with R1=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.

主权项

1. Process for the preparation of a fluorolactone derivative of the formula comprising the steps a) reacting the aldehyde of the formula with a fluoropropionate derivative of formula wherein A is selected from the chiral moieties and Ph stands for phenyl to form an aldol adduct of the formula wherein A is as above; and b) subjecting to hydrolysis the aldol adduct of formula IV to give the fluorolactone derivative of the formula I.