PROCESS FOR PRODUCING 3'-FLUOROPYRIMIDINE NUCLEOSIDES

An improved process for the synthesis of 3'-fluoropyrimidine nucleosides of the general formula: 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, r...

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Bibliographische Detailangaben
Hauptverfasser:	BOOP,DONALD CARL,US, PADMANATHAN,THURAIRAJAH,US, RIZZO,CARL J.,US, D'ANTUONO,JOSEPH,US, CLAUSS,STEVEN L.,US, CONSIDINE,JOHN LEO,US, ANDRADE,JOHN ROBERT,US
Format:	Patent
Sprache:	eng
Schlagworte:	CHEMISTRY DERIVATIVES THEREOF HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY NUCLEIC ACIDS NUCLEOSIDES NUCLEOTIDES ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS SUGARS
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Zusammenfassung:	An improved process for the synthesis of 3'-fluoropyrimidine nucleosides of the general formula: 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.