Patent ID: 6642367
Filing Date: 2003-11-04
Classification: A61P,C07H,Y02P

Abstract:
A process for the synthesis of a 2â€²-O-substituted pyrimidine nucleoside of formula: wherein:Q is a pyrimidine base or a 2-S pyrimidine base; R1 is substituted or unsubstituted C1-C30 alkyl, C1-C30 alkenyl, C1-C30 alkynyl, C6-C14 aryl, or C7-C30 aralkyl, wherein said substitution is halo, amino, hydroxyl, thiol, ether or thioether; and R2 and R3 are independently hydrogen or a hydroxyl protecting group; comprising the steps of: providing a 2-2â€²-anhydropyrimidine nucleoside; selecting an alcohol of the formula R1â€”OH; and treating said 2-2â€²-anhydropyrimidine nucleoside and said alcohol with a di or trivalent hard acid under conditions of time, temperature and pressure effective to yield said 2â€²-O-substituted pyrimidine nucleoside.