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刘丽, 王陈, 柳立新, 季婷婷. 镇痛药喷他佐辛的合成工艺改进[J]. 中国药科大学学报, 2018, 49(5): 568-571. DOI: 10.11665/j.issn.1000-5048.20180508
引用本文: 刘丽, 王陈, 柳立新, 季婷婷. 镇痛药喷他佐辛的合成工艺改进[J]. 中国药科大学学报, 2018, 49(5): 568-571. DOI: 10.11665/j.issn.1000-5048.20180508
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LIU Li, WANG Chen, LIU Lixin, JI Tingting. Improved synthesis of analgesic pentazocine[J]. Journal of China Pharmaceutical University, 2018, 49(5): 568-571. DOI: 10.11665/j.issn.1000-5048.20180508
Citation: LIU Li, WANG Chen, LIU Lixin, JI Tingting. Improved synthesis of analgesic pentazocine[J]. Journal of China Pharmaceutical University, 2018, 49(5): 568-571. DOI: 10.11665/j.issn.1000-5048.20180508
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镇痛药喷他佐辛的合成工艺改进

Improved synthesis of analgesic pentazocine

    摘要
  • 摘要: 研究喷他佐辛的合成新工艺。以3，4-二甲基吡啶和苄基氯为起始原料，经季铵化、格式加成/还原/成盐一锅法、环合、常压氢化、烷基化、精制得到目标化合物喷他佐辛。改进后的工艺操作简单，总收率达到8.4%(以3，4-二甲基吡啶的摩尔质量计)，产物纯度达到99.97%，该合成路线适合工业化生产。

     

    Abstract: A new synthetic process of pentazocine has been developed. Starting from 3, 4-dimethylpyridin and benzyl chloride, via quaternarization, Grignard reaction addition/reduction/salt, cyclization, hydrogenation, alkylation and recrystallization, pentazocine were obtained in a total yield of 8. 4%(with a molar mass of 3, 4-dimethylpyridin), with purity greater than 99. 97%. The improved synthetic route is suitable for industrial production.

     

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