| 溴夫定的合成路线改进 |
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| 引用本文： | 吴旭锋,柴世英,刘建红,王智慧,银瑞峰,曹瑞伟,孙新强.溴夫定的合成路线改进[J].中国药科大学学报,2022,53(1):41-45. |
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| 作者姓名： | 吴旭锋 柴世英 刘建红 王智慧 银瑞峰 曹瑞伟 孙新强 |
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| 作者单位： | 浙江医药股份有限公司新昌制药厂，绍兴 312500,浙江医药股份有限公司新昌制药厂，绍兴 312500,浙江医药股份有限公司新昌制药厂，绍兴 312500,浙江医药股份有限公司新昌制药厂，绍兴 312500,浙江医药股份有限公司新昌制药厂，绍兴 312500,浙江昌海制药有限公司，绍兴 312366,浙江昌海制药有限公司，绍兴 312366 |
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| 摘 要： | 通过对专利与文献报道的溴夫定合成工艺路线进行分析,采用以2'-脱氧尿苷为起始物料通过碘代、偶联、水解、脱羧溴代等4步反应和一步精制得到溴夫定的合成工艺路线,对各步反应和后处理条件进行系统优化,提高了收率,简化操作过程,使其更适合工业化生产,优化后的收率及产品纯度均高于已有文献报道.
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| 关 键 词： | 溴夫定 合成 工艺改进 |
| 收稿时间： | 2021/2/10 0:00:00 |
| 修稿时间： | 2022/1/3 0:00:00 |
Improvement of synthetic route of brivudine |
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| WU Xufeng,CHAI Shiying,LIU Jianhong,WANG Zhihui,YIN Ruifeng,CAO Ruiwei and SUN Xinqiang.Improvement of synthetic route of brivudine[J].Journal of China Pharmaceutical University,2022,53(1):41-45. |
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| Authors: | WU Xufeng CHAI Shiying LIU Jianhong WANG Zhihui YIN Ruifeng CAO Ruiwei and SUN Xinqiang |
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| Institution: | (Zhejiang Medicine Co.,Ltd.,Xinchang Pharmaceutical Factory,Shaoxing 312500;Zhejiang Changhai Pharmaceutical Co.,Ltd.,Shaoxing 312366,China) |
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| Abstract: | This article summarizes and analyzes the reported synthetic routes of brivudine in patent and literature.2′-Deoxyuridine was employed as starting material,affording brivudine through iodization,heck coupling,hydrolysis,decarboxylation,bromination and recrystallization.After optimization of reaction conditions of each step,a synthetic route suitable for industrial production was achieved with simple synthetic process,high yield and excellent purity. |
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| Keywords: | brivudine synthesis process improvement |
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