EFFICIENT NUCLEOTIDE SYNTHESIS

摘要

In one aspect, an improved synthesis for the anticancer drug tezacitabine comprises a hydroxyl deprotection reaction of vinyl stannane at a temperature of 45°C or greater, preferably about 55°C. In another aspect, the aqueous reaction product of hydroxyl deprotection is passed through a carbon filter prior to water crystallization to recover tezacitabine monohydrate from the aqueous medium. The process of the present invention significantly improves efficiency by greatly reducing the amount of time required for the synthesis of tezacitabine, and also provides improved product yields.