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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.

Inventors:
ZONG ZAIWEI (CN)
ZHAO QIAN (CN)
YANG RUIFENG (CN)
LI GAN (CN)
YI CHAO (CN)
ZHU HAIXI (CN)
Application Number:
CN2017/117596
Publication Date:
June 28, 2018
Filing Date:
December 21, 2017
Export Citation:
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Assignee:
JIANGSU AOSAIKANG PHARM CO LTD (CN)
International Classes:
C07H19/12; C07H1/00
Domestic Patent References:
WO2010017547A12010-02-11
WO1998017281A11998-04-30
Foreign References:
CN101307084A2008-11-19
Attorney, Agent or Firm:
NANJING TIANHUA PATENT AGENT CO., LTD. (CN)
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