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Silyl linker for solid-phase synthesis of nucleic acid

外国特許コード F110003372
整理番号 A251-12WO
掲載日 2011年6月23日
出願国 アメリカ合衆国
出願番号 59026705
公報番号 20080051571
公報番号 7786296
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28日(2008.2.28)
公報発行日 平成22年8月31日(2010.8.31)
国際出願番号 JP2005002059
国際公開番号 WO2005080404
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2004-049303 (2004.2.25) JP
  • 2005WO-JP02059 (2005.2.10) WO
発明の名称 (英語) Silyl linker for solid-phase synthesis of nucleic acid
発明の概要(英語) (US7786296)
The purpose of the invention is to develop a silyl linker that can be efficiently introduced on a solid-phase support used for the synthesis of nucleic acid oligomers such as DNA.
The present invention relates to a silyl linker for use in the solid-phase synthesis of nucleic acid, comprised of a compound of the general formula or its ester or salt: H—(R1)Si(R2)-(C6H4)—CONH-(A)-COOH  (I) wherein each of R1 and R2 is an alkyl or aryl group, and (A) represents a spacer moiety; a 3′-end nucleoside unit having said compound linked via an oxygen atom to the 3-position of a sugar of the nucleoside or its derivative, a solid-phase support having the 3′-end nucleoside unit, and a method for synthesis of nucleic acid oligomer with the use of said solid-phase support.
特許請求の範囲(英語) [claim1]
1. A silyl linker for use in the solid-phase synthesis of nucleic acid, comprised of a compound of the general formula or its ester or salt:
H -- (R1)Si(R2)-(C6H4) -- CONH-(A)-COOH (I)
wherein the benzene ring structure is optionally further substituted, each of R1 and R2 is an alkyl, and
(A) is an alkylene group represented by the formula -- (CH2)n -- wherein n is 2-18.
[claim2]
2. The compound according to claim 1 wherein R1 and R2 are an alkyl group having 1 to 5 carbon atoms.
[claim3]
3. The compound according to claim 1 wherein the benzene ring structure ( -- (C6H4) -- ) has a substituent.
[claim4]
4. The compound according to claim 3 wherein the substituent of the benzene ring structure is selected from the group consisting of alkyl having 1 to 4 carbon atoms, halogeno, nitro, cyano and methoxy groups.
[claim5]
5. A 3'-end nucleoside unit having the compound according to claim 1 linked via an oxygen atom to the 3-position of a sugar of a nucleoside or its derivative.
[claim6]
6. The 3'-end nucleoside unit according to claim 5 wherein a base constituting the nucleoside is thymine.
[claim7]
7. The compound according to claim 6 which is 5'-O-(4,4'-dimethoxytrityl)-thymidine-3'-O-diisopropylsilyl-4-benzoylaminobutanoic acid triethylammonium.
[claim8]
8. A solid-phase support having the 3'-end nucleoside unit according to claim 5 introduced thereon.
[claim9]
9. The solid-phase support according to claim 8 having the 3'-end nucleoside unit at a ratio of 20-30 mu mol/g.
[claim10]
10. The solid-phase support according to claim 8 or 9, which is a highly cross-linked polystyrene (HCP) solid-phase support.
  • 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)
米国特許分類/主・副
  • C07F007/08H
  • C07H019/073
  • C07H019/173
  • C07H021/04
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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