2'-0-trisubstituted silyloxymethyl-ribonucleoside-derivative...

C - Chemistry – Metallurgy – 07 – H

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C07H 19/00 (2006.01) C07F 7/18 (2006.01) C07H 21/00 (2006.01)

Patent

CA 2505266

The invention provides ribonucleoside derivatives with novel protecting groups and methods for the preparation of such ribonucleoside derivatives. The general formula (I) of the ribonucleoside derivatives is: wherein R1 is a base of the purine- or pyrimidine-family or a derivative of such a base or any other residue with serves as a nucleobase surrogate, R2 is a proton or a substituted derivative of phosphonic acid, R3 is a proton or a protection- group for the oxygen atom in 5~-position, R4, R5 and R6 are independently alkyl or aryl or a combination of alkyl and aryl or heteroatom, R4, R5 or R6 may also be cyclically connected to each other; and wherein at least one of the R4, R5 or R6 substituents comprises a tertiary C-atom or a heteroatom vicinal to the Si-atom.

L'invention concerne des dérivés de ribonucléosides et de nouveaux groupes et procédés de protection pour la préparation de ces dérivés. Dans la formule générale des dérivés de ribonucléosides, R¿1? représente une base de la famille purique ou pyrimidine ou un dérivé d'une telle base ou tout autre résidu servant de substitut de nucléobase, R¿2? représente un proton ou un dérivé substitué d'acide phosphonique, R¿3? représente un proton ou un groupe de protection pour la position 5', R¿4?, R¿5? et R¿6? représentent de manière indépendante alkyle ou aryle ou une combinaison d'alkyle et d'aryle ou un hétéroatome et peuvent également être reliés les uns aux autres de manière cyclique ; et au moins un des substituants de R¿4?, R¿5? ou R¿6? comprend un atome de C tertiaire ou un hétéroatome à proximité de l'atome de Si.

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