2'-deoxy-2'-fluorocoformycin and stereoisomers thereof

Details 2'-deoxy-2'-fluorocoformycin and stereoisomers thereof 2'-deoxy-2'-fluorocoformycin and stereoisomers thereof

C - Chemistry, Metallurgy

07

H

C07H 19/23 (2006.01) C07H 5/00 (2006.01) C07H 5/02 (2006.01) C07H 5/06 (2006.01) C07H 11/00 (2006.01) C07H 19/04 (2006.01) C07H 19/052 (2006.01)

Patent

CA 2122815

2'-Deoxy-2'-fluorocoformycin and 2'-deoxy-8-epi-2'- fluorocoformycin are synthesized in this invention through a multi-stage process via 3,5-di-O-benzoyl-2-deoxy-2- fluoro-.alpha.- and -.beta.-D-ribofuranosyl bromides. Further, according to this invention, 2'-deoxy- 2'-epi-2'-fluorocoformycin and 2'-deoxy-8,2'-diepi-2'- fluorocoformycin are synthesized by a multi-stage process starting from 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.-D- arabinofuranosyl bromide. These four 2'-fluoro derivatives of coformycin are novel compounds and have high enzyme-inhibitory activities against adenosine deaminase. In particular, these novel compounds are useful substances which exhibit therapeutic effects on acute lymphocytic leukemias due to their high enzyme-inhibitory activities above-mentioned. In addition, a variety of intermediates are obtained as novel compounds which are useful for the synthesis of the aforesaid novel 2'-fluoro derivatives of coformycin.

Dans le cadre de la présente invention, de la déoxy-2'-fluoro-2'-coformycine et de la déoxy-2'-épi-8-fluoro-2'-coformycine sont synthétisées par l'intermédiaire d'un procédé multi-étapes faisant intervenir les bromures de di-O-benzoyl-3,5-déoxy-2-fluoro-2-alpha- et -bêta-D-ribofuranosyle. De plus, conformément à la présente invention, la déoxy-2'-épi-2'-fluoro-2'-coformycine et la déoxy-2'-diépi-8,2'-fluoro-2'-coformycine sont synthétisées au moyen d'un procédé multi-étapes ayant comme point de départ le bromure de di-O-benzoyl-3,5-déoxy-2-fluoro-2-alpha-D-arabinofuranosyle. Ces quatre dérivés fluoro-2' de la coformycine sont des nouveaux composés et possèdent une activité inhibitrice élevée à l'égard de l'adénosine-désaminase. En particulier, ces nouveaux composés sont des substances utiles qui ont des effets thérapeutiques sur les leucémies aiguës lymphoblastiques en raison de cette activité inhibitrice. En outre, on obtient une variété d'intermédiaires comme composés nouveaux qui sont utiles pour la synthèse des nouveaux dérivés fluoro-2' de la coformycine.

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