Process for the preparation of 3'-fluoropyrimidine nucleosides

Details Process for the preparation of 3'-fluoropyrimidine nucleosides Process for the preparation of 3'-fluoropyrimidine nucleosides

C - Chemistry, Metallurgy

07

H

C07H 19/073 (2006.01) C07H 19/06 (2006.01)

Patent

CA 2059249

31,431-00 PROCESS FOR THE PREPARATION OF 3'-FLUOROPYRIMIDINE NUCLEOSIDES AB8TRACT An improved process for the synthesis of 3'-fluoropyrimidine nucleosides of the general formula: Image (I) by reacting a 5'-methanesulfonyl-2'-dideoxy-2,3' -anhydropyrimidine nucleoside at a concentration of up to 20% with hydrogen fluoride in the presence of a suitable aluminum reagent, recovering the 5'-methanesulfonyl-2',3'-dideoxy-3'-fluoropyrimidine nucleoside intermediate by direct crystallization and removing the 5'-methanesulfonyl protecting group in a single step by reaction with an aqueous base solution.

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