| 阿苯达唑体内活性代谢物—亚砜的制备 |
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| 引用本文： | 谢剑华,胡永洲. 阿苯达唑体内活性代谢物—亚砜的制备[J]. 浙江大学学报(医学版), 2002, 31(1): 45-46 |
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| 作者姓名： | 谢剑华 胡永洲 |
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| 作者单位： | 浙江大学药学院,浙江,杭州,310031 |
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| 摘 要： | 目的：探索阿苯达唑体内活性代谢物亚砜的制备方法。方法：通过对温度、溶剂、氧化剂、反应时间、杂质等方面的考察，确定较适当的反应条件。结果：用过碘酸钠作氧化剂，冰醋酸为溶剂，在低温下进行，反应有较好的选择性，无杂质阿苯达唑砜的存在，收率在90％以上，含量在98％以上。结论：阿苯达唑亚砜的制备可采用选择性氧化。
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| 关 键 词： | 阿苯达唑 亚砜 化学合成 活性 代谢物 |
| 文章编号： | 1008-9292(2002)01-0045-02 |
| 修稿时间： | 2000-03-09 |
Preparation of albendazole sulfoxide—an active metabolite |
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| XIE Jian hua,HU Yong zhou. Preparation of albendazole sulfoxide—an active metabolite[J]. Journal of Zhejiang University. Medical sciences, 2002, 31(1): 45-46 |
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| Authors: | XIE Jian hua HU Yong zhou |
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| Abstract: | Objective: To investigate the facile method for preparation of albendazole sulfoxide,an active metabolite in vivo . Methods: The reaction condition was investigated according to evaluations to the results of the experiment through temperature,solvent,oxidation agent,reaction time and impurity. Results: The target compound was obtained by oxidation of albendazole with the presence of sodium metaperiodate in glacial acetic acid under low temperature and was free from contamination by impurity albendazole sulfone.Pure product (content>98%) and high yield (>90%) have been achieved due to reaction selection. Conclusion: Oxidation condition is essential to the preparation of albendazole sulfoxide. |
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| Keywords: | Albendazole sulfoxide/chem syn |
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