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Silyl linker for solid-phase synthesis of nucleic acid

Foreign code F110003372
File No. A251-12WO
Posted date Jun 23, 2011
Country United States of America
Application number 59026705
Gazette No. 20080051571
Gazette No. 7786296
Date of filing Feb 10, 2005
Gazette Date Feb 28, 2008
Gazette Date Aug 31, 2010
International application number JP2005002059
International publication number WO2005080404
Date of international filing Feb 10, 2005
Date of international publication Sep 1, 2005
Priority data
  • P2004-049303 (Feb 25, 2004) JP
  • 2005WO-JP02059 (Feb 10, 2005) WO
Title Silyl linker for solid-phase synthesis of nucleic acid
Abstract (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.
Scope of claims [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.
  • Inventor, and Inventor/Applicant
  • SEKINE MITSUO
  • SEIO KOHJI
  • OHKUBO AKIHIRO
  • JAPAN SCIENCE AND TECHNOLOGY AGENCY
IPC(International Patent Classification)
Reference ( R and D project ) CREST Creation of Bio-Devices and Bio-Systems with Chemical and Biological Molecules for Medical Use AREA
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