[EN] PROCESSES FOR PREPARING 2-DIHALO RIBOLACTONES<br/>[FR] PROCÉDÉS DE PRÉPARATION DE 2-DIHALO-RIBOLACTONES
申请人:COCRYSTAL PHARMA INC
公开号:WO2017075590A2
公开(公告)日:2017-05-04
Methods for forming 2-bromo, 2-fluoro ribofuranose intermediates and 2-chloro, 2- fluoro ribofuranose intermediates for use in preparing antiviral nucleosides are disclosed. Methods for forming nucleosides, and nucleoside prodrugs, using the intermediates, are also disclosed. The methods all produce intermediates, and the resulting nucleosides and prodrugs thereof, wherein the chirality of the carbon at the 2-position is controlled. In some embodiments, the chemistry involves using chiral auxiliaries, such as (R)-2,2-dimethyl-l,3- dioxolane-4-carbaldehyde, and in other embodiments, the chemistry involves using chiral starting materials, such as D-xylose.