1-.alpha.-halo-2,2-difluoro-2-deoxy-d-ribofuranose...

Details 1-.alpha.-halo-2,2-difluoro-2-deoxy-d-ribofuranose... 1-.alpha.-halo-2,2-difluoro-2-deoxy-d-ribofuranose...

C - Chemistry, Metallurgy

07

H

C07H 3/08 (2006.01)

Patent

CA 2574954

1-.alpha.-halo-2,2-difluoro-2-deoxy-D-ribofuranose derivative of formula (I) having the 3-hydroxy group protected with a biphenylcarbonyl group is a solid which can be easily purified by a simple procedure such as recrystallization, and therefore, it can be advantageously used as an intermediate in the preparation of gemcitabine in a large scale. Further, the 1-.alpha.-halo-2,2-difluoro-2-deoxy- D- ribofuranose derivative of formula (I) can be prepared with high stereoselectivity using the compound of formula (V) as an intermediate. Chemical structures of Formulas (I) and (V) are as follows: (see formula I) (see formula V) wherein, R1 is benzoyl or (see formula II); R2 is hydrogen, cyano, halogen, carboalkoxy, nitro, C1-2 alkoxy, C1-2 alkyl or dialkylamino; X is Cl, Br or I; and R3 is methyl, ethyl or phenyl.

L'invention concerne un dérivé de 1-a-halo-2,2-difluoro-2-désoxy-D-ribofuranose de formule (I) dont le groupe 3-hydroxy est protégé par un groupe biphénylcarbonyle étant un solide pouvant être purifié facilement au moyen d'une simple procédure, telle que la recristallisation et pouvant être utilisé, par conséquent, de manière avantageuse comme intermédiaire dans la préparation de gémcitabine à grande échelle. De plus, le dérivé de 1-a-halo-2,2-difluoro-2-désoxy-D-ribofuranose de formule (I) peut être préparé avec une stéréosélectivité élevée au moyen du composé de formule (V) comme intermédiaire.

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