DERIVATIVES OF 1-α-HALOGEN-2,2-DIFLUORO-2-DEOXY-D-RIBOFURANOSE AND METHOD OF THEIR OBTAINMENT Russian patent published in 2009 - IPC C07H5/02 C07H1/00 C07H11/04 

Abstract RU 2346948 C2

FIELD: chemistry.

SUBSTANCE: invention claims derivatives of 1-α-halogen-2,2-difluoro-2-deoxy-D-ribofuranose of the general formula (I) in solid state, where R1 is benzoyl or ; R2 is hydrogen; and X is CI, Br or I; which can be applied as intermediates in stereoselective method of gemcitabine obtainment. In addition, invention claims stereoselective method of obtaining compounds of the general formula (I), including stages of: (i) recovery of 1-oxoribose of formula to obtain lactol of formula ; (ii) interaction of compound of formula (III) with halogen phosphate compound of formula in the presence of a base to obtain 1-phosphatefuranose derivative of formula ; and (iii) interaction of compound of formula (V) (also included in the claim) with halogen source, with further recrystallisation of obtained product; where R1, R2 and X are the same as indicated above while R3 is phenyl.

EFFECT: efficient method of obtaining derivatives of the abovementioned agent.

11 cl, 6 ex

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RU 2 346 948 C2

Authors

Li Dzaekheon

Park Ga Seung

Li Moonsub

Kim Khan Kiong

Bang Khio-Dzeong

Chang Jang-Kil

Li Gvan Sun

Dates

2009-02-20Published

2005-06-21Filed