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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. DOI: 10.11665/j.issn.1000-5048.20220106
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. DOI: 10.11665/j.issn.1000-5048.20220106
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WU Xufeng, CHAI Shiying, LIU Jianhong, WANG Zhihui, YIN Ruifeng, CAO Ruiwei, SUN Xinqiang. Improvement of synthetic route of brivudine[J]. Journal of China Pharmaceutical University, 2022, 53(1): 41-45. DOI: 10.11665/j.issn.1000-5048.20220106
Citation: WU Xufeng, CHAI Shiying, LIU Jianhong, WANG Zhihui, YIN Ruifeng, CAO Ruiwei, SUN Xinqiang. Improvement of synthetic route of brivudine[J]. Journal of China Pharmaceutical University, 2022, 53(1): 41-45. DOI: 10.11665/j.issn.1000-5048.20220106
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溴夫定的合成路线改进

Improvement of synthetic route of brivudine

    摘要
  • 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。

     

    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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