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公开(公告)号：US10752652B2
公开(公告)日：2020-08-25
申请号：US16465418
申请日：2017-12-21
发明人： Zaiwei Zong , Qian Zhao , Ruifeng Yang , Gan Li , Chao Yi , Haixi Zhu
摘要： A method for preparing a β-nucleoside compound, including the following steps: 1) performing a silylation reaction of a nitrogenous base or an analogue thereof in the presence of TMSOTf to give 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 hydroxyl protecting group to give a closed β-nucleoside compound; and 3) performing a deprotection reaction to give the β-nucleoside compound. The method uses a one-pot process to prepare the key intermediates of the β-nucleoside compound, and the yield of materials in β-configuration increases significantly. The method has the benefits of simple operations, being energy conservation and environment protection, and being suitable for industrial applications.
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