| 引用本文: | 褚定军,谢晓强.倍他米松环氧物开环氟化的工艺研究[J].中国现代应用药学,2020,37(13):1602-1605. |
| CHU Dingjun,XIE Xiaoqiang.Study on the Process of Ring-opening Fluorination of Betamethasone Epoxide[J].Chin J Mod Appl Pharm(中国现代应用药学),2020,37(13):1602-1605. |
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| 摘要: |
| 目的 改进制备倍他米松的关键步骤开环氟化，解决传统工艺中氟代试剂存在废液多等缺点。方法 对多种氟代试剂进行筛选，进一步考察了反应溶剂、温度、HF浓度等对反应的影响。结果 优选出HF-[Bmim]OTf复合物作为开环氟化试剂，获得倍他米松环氧物开环氟化的较优条件。溶剂甲苯和离子液体催化剂[Bmim]OTf可回收套用，降低了开环氟化的生产成本和含氟废水的排放量。结论 该工艺具备工业化生产的潜力。 |
| 关键词: 倍他米松环氧物 氟化氢 [Bmim]OTf 开环氟代反应 |
| DOI：10.13748/j.cnki.issn1007-7693.2020.13.012 |
| 分类号:R914.4 |
| 基金项目: |
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| Study on the Process of Ring-opening Fluorination of Betamethasone Epoxide |
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CHU Dingjun, XIE Xiaoqiang
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Aurisco Pharmaceutical Co., Ltd., Taizhou 317200, China
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| Abstract: |
| OBJECTIVE To improve the key step of ring-opening fluorination in the preparation of betamethasone, to resolve the shortcomings of the traditional fluorination agent, which will produce large amount of waste liquid. METHODS Screening different fluorination agents, and the optimal conditions for ring-opening fluorination were achieved by investigating reaction solvent, temperature, concentration of HF, and so on. RESULTS The HF-[Bmim]OTf complex was chosen as favorable fluorination agents, the optimal ring-opening fluorination of betamethasone epoxide was obtained. The solvent toluene and ionic liquid[Bmim]OTf could be recycled in this process, which dramatically reduced the production cost and the amount of polluted fluorine-containing waste water. CONCLUSION The process has the potential for the industrial production of betamethasone. |
| Key words: betamethasone epoxide HF [Bmim]OTf ring-opening fluorination |
