3'-end nucleoside unit comprising phosphoramidite

C - Chemistry – Metallurgy – 07 – H

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Details

C07H 21/04 (2006.01) C07F 9/6558 (2006.01) C07F 9/6561 (2006.01) C12N 15/11 (2006.01)

Patent

CA 2556594

It is intended to provide a method of binding a 3~-terminal nucleoside to a hydroxyl group on a solid phase under the same conditions as in a DNA chain extension reaction. A 3~-terminal nucleoside unit containing phosphoramidite which is a compound represented by the following general formula (I): (N)-O- (R1)Si(R2)-(C6H4)-(CH2)n-O-P(OR3)N(R4)(R5) wherein (N) stands for an arbitrary nucleoside or its derivative; R1, R2, R4 and R5 are each an alkyl group or an aryl group; R3 is a phosphate-protecting group; and n is an integer of from 1 to 5; a solid phase support having a 3~-terminal nucleoside unit, which is the above compound, transferred thereinto; and a method of synthesizing a nucleic acid oligomer with the use of this solid phase support.

Il est prévu fournir un procédé consistant à lier un nucléoside de terminaison 3~à un groupement hydroxyle sur une phase solide dans les mêmes conditions que dans une réaction d'extension de chaîne d'ADN. Une unité de nucléoside de terminaison 3~contenant un phosphoramidite qui est un composé représenté par la formule générale suivante (I) : (N)-O-(R1)Si(R2)-(C¿6?H¿4?)-(CH¿2?)¿n?-O-P(OR3)N(R4)(R5) (I) dans laquelle (N) représente un nucléoside arbitraire ou son dérivé, R1, R2, R4 et R5 représentent chacun un groupement alkyle ou un groupement aryle, R3 représente un groupement de protection de phosphate et n est un nombre entier de 1 à 5, un support en phase solide comportant une unité de nucléoside de terminaison 3~, qui est le composé ci-dessus, transférée dans celui-ci, et un procédé de synthèse d'un oligomère d'acide nucléique grâce à l'utilisation de ce support en phase solide.

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