Title:
核酸保護基の導入方法
Document Type and Number:
Japanese Patent JP5168145
Kind Code:
B2
Abstract:
It is an object of the invention to provide a simple and economical method for introducing the following substituent (I) at the 2'-hydroxyl group of the ribose of a ribonucleic acid derivative whose 3'-hydroxyl group and 5'-hydroxyl group are protected with a silicon protecting group:
[in formula (I), WG 1 represents an electron-withdrawing group] and to provide a method for producing a ribonucleic acid derivative represented by the following general formula (3), comprising the reaction of a ribonucleic acid derivative represented by the following general formula (1) with a monothioacetal compound represented by the following general formula (2) to produce the ribonucleic acid derivative represented by the following general formula (3), using iodine as the reagent for halogenating the sulfur atom of the monothioacetal compound (2) in the presence of an acid:
[in formulae (1), (2), and (3), Bz represents a nucleobase which may or may not have a protecting group; WG 1 represents an electron-withdrawing group; R 3 represents alkyl or aryl; and A represents a silicon substituent].
Inventors:
Hidetoshi Kitagawa
Uetake Koichi
Uetake Koichi
Application Number:
JP2008527773A
Publication Date:
March 21, 2013
Filing Date:
August 01, 2007
Export Citation:
Assignee:
NIPPON SHINYAKU CO.,LTD.
International Classes:
C07H23/00; C07H19/10; C07H19/20; C07H21/02
Foreign References:
| WO2002088062A1 | 2002-11-07 | |||
| WO2002054931A2 | 2002-07-18 | |||
| WO2006022323A1 | 2006-03-02 | |||
| WO2002088062A1 | 2002-11-07 | |||
| WO2002054931A2 | 2002-07-18 |
Attorney, Agent or Firm:
Naoto Shimizu