Synthetic intermediates of 2-alkynyladenosines, processes...

C - Chemistry – Metallurgy – 07 – H

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260/229.5

C07H 19/06 (2006.01) C07H 19/16 (2006.01)

Patent

CA 2035038

The present invention relates to a novel compound represented by the following formula [I] which is useful as a synthetic intermediate of a 2-alkynyladenosine. The present invention also relates to a process for producing the compound and a process for producing a 2-alkynyladenosine [IV] by way of the compound. Further, the present invention relates to a 2-alkynyladenosine derivative represented by the following formula [V] having excellent storage stability and, to a method of storing the 2-alkynyladenosine in the form of that derivative. (see fig. I) [I] A = a leaving group, [II] A = NH2, [V] A = NHR4, wherein R1 through R4 represent a hydrogen atom or a protective group, and n denotes an integer of 1 to 15, provided that R1 through R4 do not represent a hydrogen atom simultaneously.

Cette invention a trait à un nouveau composé représenté par la formule [I] qui est utile comme intermédiaire synthétique d'une 2-alkynyladénosine. La présente invention concerne également un procédé pour produire le composé et un procédé pour produire une 2-alkynyladénosine [IV] au moyen du composé. Cette invention a en outre trait à un dérivé d'une 2-alkynyladénosine représenté par la formule suivante [V] et ayant une excellente stabilité d'entreposage et, à une méthode d'entreposage de la 2-alkynyladénosine sous la forme dudit dérivé. (Voir fig. I) [I] A = un groupe partant, [II] A = NH2, [V] A = NHR4, où R1 à R4 représentent un atome d'hydrogène ou un groupe protecteur, et n réfère à un nombre entier de 1 à 15 15, à condition que R1 à R4 ne représentent pas simultanément un atome d'hydrogène.

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