环丙基乙炔的合成研究
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Study on the Synthesis of Cyclopropyl Acetylene
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    摘要:

    以环丙基甲基酮为起始原料,五氯化磷为氯化试剂,采用先氯化后消除的工艺合成了依非韦伦关键中间体环丙基乙炔。针对二氯代物中间体和一氯代物中间体消除反应活性的不同,分别在三乙胺和氢氧化钾存在下进行分步消除反应,以环丙基甲基酮计,环丙基乙炔单程收率可达49%。同时建立了三乙胺的回收套用工艺,进一步降低了成本,具有良好的工业化前景。

    Abstract:

    Using cyclopropyl methyl ketone as starting material and phosphorus pentachloride as chlorination reagent, cyclopropyl acetylene, the key intermediate of Efavirenz, was synthesized by chlorination followed by elimination. Aiming at the different eliminating reactivity between the dichloride and monochloride intermediates, the stepwise elimination reactions were carried out in the presence of triethylamine and potassium hydroxide, respectively. A one-way yield as high as 49% of cyclopropyl acetylene was obtained based on cyclopropyl methyl ketone. At the same time, the recycling process for triethylamine has been established, which further reduces the cost and has good prospects for industrialization.

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张洁,陈亚红,田丰收,王瑞勇.环丙基乙炔的合成研究[J].精细化工,2019,36(10):

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  • 收稿日期:2019-03-01
  • 最后修改日期:2019-04-25
  • 录用日期:2019-04-25
  • 在线发布日期: 2019-09-06
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