Phosphoramidite compound and method for producing oligo-rna

C - Chemistry – Metallurgy – 07 – H

Patent

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Details

C07H 19/067 (2006.01) C07C 255/13 (2006.01) C07H 19/167 (2006.01) C07H 21/02 (2006.01)

Patent

CA 2577922

Disclosed is a novel phosphoramidite compound which is useful for synthesis of an oligo-RNA. Specifically disclosed is a phosphoramidite compound represented by the following general formula (1). [In the formula, Bx represents a nucleic acid base which may have a protecting group; R1 represents a substituent represented by the following general formula (2): (wherein R11, R12 and R13 may be the same or different and respectively represent a hydrogen or an alkoxy); R2a and R2b may be the same or different and respectively represent an alkyl or form a 5-6 membered saturated amino ring group together with an adjacent nitrogen atom, and the saturated amino ring group may have an oxygen atom or a sulfur atom as a ring-forming atom other than the nitrogen atom; and WG1 and WG2 may be the same or different and respectively represent an electron-withdrawing group.]

L~invention porte sur un nouveau composé de phosphoramidite servant à la synthèse d~un oligo-ARN. L~invention porte spécifiquement sur un composé de phosphoramidite représenté par la formule générale suivante (1). (1) [Dans la formule, Bx représente une base acide nucléique qui peut avoir un groupe de protection ; R1 représente un élément substitutif représenté par la formule générale suivante (2) : (2) (où R11, R12 et R13 peuvent être les mêmes ou différents et représentent respectivement un hydrogène ou un alcoxy) ; R2a et R2b peuvent être les mêmes ou différents et représentent respectivement un alkyle ou forment un groupe annulaire amino saturé à 5 ou 6 éléments avec un atome d~azote adjacent, et le groupe annulaire amino saturé peut avoir un atome d~oxygène ou un atome de soufre comme atome de formation annulaire autre que l~atome d~azote ; et WG1 et WG2 peuvent être les mêmes ou différents et représentent respectivement un groupe de prélèvement électronique.]

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