Title:
METHOD FOR PREPARING β-NUCLEOSIDE COMPOUND
Document Type and Number:
WIPO Patent Application WO/2018/113710
Kind Code:
A1
Abstract:
Provided in the present invention is a method for preparing a β-nucleoside compound, comprising the steps of: 1) performing a silylation reaction of a nitrogenous base or an analogue thereof in the presence of TMSOTf to obtain the nitrogenous base or the analogue thereof being protected by trimethylsilyl; 2) performing a direct glycosylation reaction of the reaction liquid, without being isolated, and a five- or six-membered ring saccharide or a derivative thereof closed by a hydroxy protecting group to obtain a closed β-nucleoside compound; and 3) performing a deprotection reaction to obtain the β-nucleoside compound. The method uses a one-pot process to prepare the key intermediate of the β-nucleoside compound, and the yield of the β-configuration substance increases significantly. The method has the advantages of a simple operation, saving energy and protecting the environment, and is suitable for industrial application.
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Inventors:
ZONG ZAIWEI (CN)
ZHAO QIAN (CN)
YANG RUIFENG (CN)
LI GAN (CN)
YI CHAO (CN)
ZHU HAIXI (CN)
ZHAO QIAN (CN)
YANG RUIFENG (CN)
LI GAN (CN)
YI CHAO (CN)
ZHU HAIXI (CN)
Application Number:
PCT/CN2017/117596
Publication Date:
June 28, 2018
Filing Date:
December 21, 2017
Export Citation:
Assignee:
JIANGSU AOSAIKANG PHARM CO LTD (CN)
International Classes:
C07H19/12; C07H1/00
Domestic Patent References:
WO2010017547A1 | 2010-02-11 | |||
WO1998017281A1 | 1998-04-30 |
Foreign References:
CN101307084A | 2008-11-19 |
Attorney, Agent or Firm:
NANJING TIANHUA PATENT AGENT CO., LTD. (CN)
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