Invention Grant
US09029528B2 Solution-based method of making oligonucleotides via phosphoramidite coupling
有权
通过亚磷酰胺偶联制备寡核苷酸的基于溶液的方法
- Patent Title: Solution-based method of making oligonucleotides via phosphoramidite coupling
- Patent Title (中): 通过亚磷酰胺偶联制备寡核苷酸的基于溶液的方法
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Application No.: US13473884Application Date: 2012-05-17
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Publication No.: US09029528B2Publication Date: 2015-05-12
- Inventor: Kunihiro Hirai , Satoshi Katayama
- Applicant: Kunihiro Hirai , Satoshi Katayama
- Applicant Address: JP Tokyo
- Assignee: Ajinomoto Co., Inc.
- Current Assignee: Ajinomoto Co., Inc.
- Current Assignee Address: JP Tokyo
- Agency: Oblon, McClelland, Maier & Neustadt, L.L.P.
- Priority: JP2011/110872 20110517
- Main IPC: C07H21/00
- IPC: C07H21/00 ; C07C41/16

Abstract:
A method of producing an n+p-mer oligonucleotide efficiently in a high yield, which includes use of, as a starting material, an n-mer oligonucleotide wherein the 3′-terminal hydroxyl group is protected, and the 5′-terminal hydroxyl group is protected by a temporary protecting group, and continuously performing, in a solution, (1) a deprotection step of the 5′-terminal hydroxyl group, (2) a 5′-terminal elongation step by the addition of a p-mer oligonucleotide wherein the 3′-position is phosphoramidited, and (3) an oxidation step or a sulfurization step of a phosphite triester moiety. The 3′-hydroxyl group of the n-mer oligonucleotide is protected by a solubilizing protecting group represented by formula: -L-Y—Z, where L is a group represented by formula (a1): Y is an oxygen atom, or NR wherein R is a hydrogen atom, an alkyl group or an aralkyl group, and Z is a group represented by formula (a2):
Public/Granted literature
- US20120296074A1 PRODUCTION METHOD OF OLIGONUCLEOTIDE Public/Granted day:2012-11-22
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