Login| Sign Up| Help| Contact|

Patent Searching and Data


Title:
OLIGONUCLEOTIDE MANUFACTURING METHOD
Document Type and Number:
WIPO Patent Application WO/2017/111137
Kind Code:
A1
Abstract:
An objective of the present invention is to provide a method for stably and efficiently manufacturing oligonucleotides, in particular oligonucleotides formed having various functional groups connected to the 3' terminal. An oligo nucleic acid having the 3' terminal protected by a silyl protecting group has the 3' terminal selectively deprotected under desilylation conditions that do not affect protecting groups other than silyl groups. The present invention can more efficiently manufacture oligonucleotides by an oligonucleotide manufacturing method comprising a step in which a phosphorodiamidite reagant is used to apply phosphitylation conditions that do not affect the protecting groups on the oligo nucleic acid, and after obtaining a phosphoramidited 3' terminal oligonucleotide, which is represented by formula (Ia-1)(definitions for the symbols are as set forth in the description), a functional group is connected, either directly or via a linker, to the 3' terminal of said phosphoramidited 3' terminal oligonucleotide to obtain an oligonucleotide having a functional group at the 3' terminal and represented by formula (Ia-2)(definitions for the symbols are as set forth in the description).

Inventors:
YAMASHITA KEN (JP)
HIRAI KUNIHIRO (JP)
KATAYAMA SATOSHI (JP)
ICHIMARU TAISUKE (JP)
TAKAHASHI DAISUKE (JP)
HIROSE NAOKO (JP)
Application Number:
PCT/JP2016/088580
Publication Date:
June 29, 2017
Filing Date:
December 22, 2016
Export Citation:
Click for automatic bibliography generation   Help
Assignee:
AJINOMOTO KK (JP)
International Classes:
C07H21/04
Domestic Patent References:
WO2011061114A12011-05-26
WO2000000499A12000-01-06
WO2015168172A12015-11-05
WO2013022966A12013-02-14
WO2012024776A12012-03-01
WO2011156202A12011-12-15
WO2011005861A12011-01-13
WO2014077292A12014-05-22
WO2013122236A12013-08-22
WO2012157723A12012-11-22
WO2005070859A12005-08-04
WO2013179412A12013-12-05
Foreign References:
JP2002255990A2002-09-11
JP2001089496A2001-04-03
JPH11322783A1999-11-24
JPH09505307A1997-05-27
JPH09505306A1997-05-27
JP2012506701A2012-03-22
JP2009524695A2009-07-02
JP2008163024A2008-07-17
US20130267697A12013-10-10
JP2012510460A2012-05-10
JP2009516521A2009-04-23
JP2010275254A2010-12-09
JP2012111728A2012-06-14
Other References:
GREENE THEODORA W ET AL.: "PROTECTIVE GROUPS IN ORGANIC SYNTHESIS", pages 77 - 86
FETTES KEVIN J. ET AL.: "Synthesis and nucleic- acid-binding properties of sulfamide- and 3'-N- sulfamate-modified DNA", JOURNAL OF THE CHEMICAL SOCIETY, PERKIN TRANSACTIONS 1, vol. 4, 2002, pages 485 - 495, XP055395813
KIM SHOKAKU ET AL.: "Liquid-Phase RNA Synthesis by Using Alkyl-Chain-Soluble Support", CHEMISTRY - A EUROPEAN JOURNAL, vol. 19, no. 26, 2013, pages 8615 - 8620, XP055211240
SHOJI TAKAO ET AL.: "Synthesis of conjugated oligonucleotide in solution phase using alkyl- chain-soluble support", CHEMISTRY LETTERS, vol. 43, no. 8, 2014, pages 1251 - 1253, XP055393419
Attorney, Agent or Firm:
TAKASHIMA, Hajime (JP)
Download PDF: