Jiangsu Aosaikang Pharmaceutical Co., Ltd.

Zaiwei Zong

Qian Zhao

Ruifeng Yang

Chao Yi

Haixi Zhu

Gan Li

A method for preparing a &#x3b2;-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 &#x3b2;-nucleoside compound; and 3) performing a deprotection reaction to give the &#x3b2;-nucleoside compound. The method uses a one-pot process to prepare the key intermediates of the &#x3b2;-nucleoside compound, and the yield of materials in &#x3b2;-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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Nanjing, China

Zaiwei Zong