METHOD OF OBTAINING 2'-DESOXY-2', 2'-DIFLUOROCYTIDINE Russian patent published in 2009 - IPC C07H1/00 C07H19/73 C07H5/02 

Abstract RU 2360919 C2

FIELD: chemistry.

SUBSTANCE: invention relates to method of obtaining enriched with β-anomer 2'-desoxy-2',2'-difluorocytidine of formula (I)

, which includes stages: (i) interaction of enriched with α-anomer compound of 1-halogenribofuranose of formula (III) with nucleic base of formula (IV) in solvent obtaining enriched with β-anomer nucleoside of formula (II) , with constant removal of formed in reaction process silylhalogenide of formula R3SiX (V) by distillation using carrier or running inert gas through reaction mixture; and (ii) removal of protective group from enriched with β-anomer nucleoside of formula (II). Invention also relates to method of obtaining hydrate of enriched with β-anomer 2'-desoxy-2',2'-difluorocytidine of formula (I), which at stage (ii) after removal of protective group additionally includes stages of dissolving formula (I) nucleoside in water; heating of obtained solution to temperature from 40 to 60°C; cooling of solution to temperature ranging from 10 to 25°C with or without mixing and without changing pH; and filtering of deposited solid substances.

EFFECT: method improvement.

17 cl, 2 tbl, 7 ex

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RU 2 360 919 C2

Authors

Li Dzaekheon

Park Ga Seung

Li Moonsub

Bang Khio-Dzeong

Li Dzae Chul

Kim Cheol Kiong

Choi Chang-Dzu

Kim Khan Kiong

Li Khoe Chul

Chang Jang-Kil

Li Gvan Sun

Dates

2009-07-10Published

2005-12-29Filed