METHOD FOR THE PREPARATION OF 2'-DEOXY-2',2'-DIFLUOROCYTIDINE

METHOD FOR THE PREPARATION OF 2'-DEOXY-2',2'-DIFLUOROCYTIDINE

This invention relates to an improved method for stereoselectively preparing 2¢~-deoxy-2¢~,2¢~-difluorocytidine of formula (I), which comprises the steps of reacting a 1-halo ribofuranose compound of formula (III) with a nucleobase of formula (IV) in a solvent to obtain a nucleoside of formula (II)...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: PARK, GHA SEUNG, LEE, JAE CHUL, KIM, CHEOL KYONG, BANG, HYO-JEONG, LEE, JAEHEON, KIM, HAN KYONG, CHANG, YOUNG-KIL, LEE, GWAN SUN, LEE, MOONSUB, CHOI, CHANG-JU, LEE, HOE CHUL
Format: Patent
Sprache:eng ; fre
Schlagworte:
CHEMISTRY
DERIVATIVES THEREOF
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
SUGARS
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Beschreibung
Zusammenfassung:This invention relates to an improved method for stereoselectively preparing 2¢~-deoxy-2¢~,2¢~-difluorocytidine of formula (I), which comprises the steps of reacting a 1-halo ribofuranose compound of formula (III) with a nucleobase of formula (IV) in a solvent to obtain a nucleoside of formula (II) with removing the silyl halide of formula (V) produced during the reaction; and deprotecting the nucleoside of formula (II) to obtain 2¢~-deoxy-2¢~,2¢~-difluorocytidine of formula (I).