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3′-end nucleoside unit comprising phosphoramidite

外国特許コード F110003373
整理番号 A251-13WO
掲載日 2011年6月23日
出願国 アメリカ合衆国
出願番号 59026805
公報番号 20080039620
公報番号 7943758
出願日 平成17年2月10日(2005.2.10)
公報発行日 平成20年2月14日(2008.2.14)
公報発行日 平成23年5月17日(2011.5.17)
国際出願番号 JP2005002058
国際公開番号 WO2005080411
国際出願日 平成17年2月10日(2005.2.10)
国際公開日 平成17年9月1日(2005.9.1)
優先権データ
  • 特願2004-049312 (2004.2.25) JP
  • 2005WO-JP02058 (2005.2.10) WO
発明の名称 (英語) 3′-end nucleoside unit comprising phosphoramidite
発明の概要(英語) (US7943758)
Methods of synthesizing nucleic acid oligomers on a solid-phase support having a 3′-end nucleoside unit introduced thereon-as represented by formula II: wherein of formula II represents a 2′-deoxyribonucleoside or its N-protected derivative, the substituent ―O―(R1)Si(R2)―(C6H3R6)―(CH2)n―O―P(OR3)XO)―(CH2)n is attached at the 3′ position of the sugar moiety of the nucleoside substituent; each of R1 and R2 is an alkyl or optionally substituted aryl group, wherein the optionally substituted aryl group has a substituent selected from the group consisting of C1-4 alkyl, nitro, cyano, halo and methoxyl; R3 is a protecting group; X is S or O; R7 is H or 4,4′-dimethoxytrityl; each n is an integer of from 1 to 5; and the solid-phase support has hydroxyl groups on its surface.
特許請求の範囲(英語) [claim1]
1. A compound represented by the following formula:
wherein
of formula I represents a 2'-deoxyribonucleoside or its N-protected derivative, the substituent -- O -- (R1)Si(R2) -- (C6H3R6) -- (CH2)n -- O -- P(OR3)N(R4)(R5) is attached at the 3' position of the sugar moiety of the nucleoside substituent; each of R1, R2, R4 and R5 is an alkyl or optionally substituted aryl group, wherein the optionally substituted aryl group has a substituent selected from the group consisting of C1-5 alkyl, nitro, cyano, halo and methoxyl; R3 is a protecting group; R6 substituent of the benzene ring -- (C6H3R6) -- is selected from the group consisting of H, C1-4 alkyl, halo, nitro, cyano and methoxyl; R7 is H or 4,4'-dimethoxytrityl; and n is an integer of from 1 to 5.
[claim2]
2. The compound according to claim 1 wherein R1 and R2 are independently a C1-5 alkyl.
[claim3]
3. The compound according to claim 1 wherein R1 and R2 are independently substituted aryl.
[claim4]
4. The compound according to any one of claims 1 to 3 wherein the protecting group R3 is 2-cyanoethyl, 4-nitrophenylethyl, N-(trifluoroacetyl)aminobutyl, or 4-[N-methyl-N-(2,2,2-trifluoroacetyl)amino]butyl.
[claim5]
5. The compound according to claim 4 wherein the protecting group R3 is 2-cyanoethyl.
[claim6]
6. The compound according to claim 1 wherein each of R4 and R5 is independently C1-4 alkyl, benzyl, phenyl, or naphthyl.
[claim7]
7. The compound according to claim 1 wherein each of R4 and R5 is independently isopropyl.
[claim8]
8. The compound according to claim 1 wherein R6 is selected from the group consisting of C1-4 alkyl, halo, nitro, cyano and methoxy.
[claim9]
9. A compound having the structure
wherein DMTr is 4,4'-dimethoxytrityl.
[claim10]
10. A compound having the structure
wherein DMTr is 4,4'-dimethoxytrityl.
[claim11]
11. A solid-phase support having a 3'-end nucleoside unit introduced thereon as represented by formula II:
wherein
of formula II represents a 2'-deoxyribonucleoside or its N-protected derivative, the substituent -- O -- (R1)Si(R2) -- (C6H3R6) -- (CH2)n -- O -- P(OR3)XO) -- (CH2)n is attached at the 3' position of the sugar moiety of the nucleoside substituent; each of R1 and R2 is an alkyl or optionally substituted aryl group, wherein the optionally substituted aryl group has a substituent selected from the group consisting of C1-4 alkyl, nitro, cyano, halo and methoxyl; R3 is a protecting group; X is S or O; R7 is H or 4,4'-dimethoxytrityl; each n is an integer of from 1 to 5; and the solid-phase support has hydroxyl groups on its surface.
[claim12]
12. The solid-phase support according to claim 11 having the 3'-end nucleoside units present at a ratio of 20-30 mu mol/g.
[claim13]
13. The solid-phase support of claim 11, wherein the solid-phase support is a highly cross-linked polystyrene (HCP).
  • 発明者/出願人(英語)
  • SEKINE MITSUO
  • SEIO KOHJI
  • OHKUBO AKIHIRO
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
国際特許分類(IPC)
参考情報 (研究プロジェクト等) CREST Creation of Bio-Devices and Bio-Systems with Chemical and Biological Molecules for Medical Use AREA
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