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β-L-2′-脱氧胞苷的合成

Synthesis ofβ-L-2′-deoxycytidine
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摘要 β-L-2′-脱氧胞苷为重要的医药中间体。以2′-脱氧-L-核糖和胞嘧啶为起始原料,通过甲苷化、酯化、氯代、水解脱保护基等步骤,以49.7%的收率合成了β-L-2′-脱氧胞苷,HPLC纯度达99.9%。产物结构经1H NMR,13C NMR和MS确证。 β-L-2′-deoxycytidine is an important pharmaceutical intermediate,and its synthesis methods are seldom disclosed at home and abroad.In this paper,taking 2′-deoxyl-ribose and cytosine as starting materials,the yield ofβ-l-2′-deoxycytidine was obtained at 49.7%through the steps of methylization,esterification,chlorination,and off-protecting group,etc.After purification,the purity of HPLC reached 99.9%.The structure of the product was confirmed by 1H NMR,13C NMR and MS.
作者 常海洲 沈开源 江霜英 CHANG Hai-zhou;SHEN Kai-yuan;JIANG Shuang-ying(College of Science, University of Shanghai for Science and Technologe, Shanghai 200093, China;College of Enviromental Science and Engineering, Tongji University, Shanghai 200092, China)
出处 《合成化学》 CAS 北大核心 2020年第8期718-721,共4页 Chinese Journal of Synthetic Chemistry
基金 国家自然科学基金资助项目(21276156)。
关键词 2′-脱氧-L-核糖 糖苷化 合成 β-L-2′-脱氧胞苷 酯化 2′-deoxy-L-ribose glycosylation synthesis β-L-2′deoxycytidine esterification
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