| 摘要: |
| 目的 探索并改进雷芬那辛的合成工艺。方法 以2-苯基苯甲酸和N-Boc-4-羟基哌啶为起始物料，经Curtius重排、亲核取代、氢化还原和缩合四步反应制得雷芬那辛(Ⅰ)。结果 该工艺的雷芬那辛收率达到63.4%，并经HRMS、1H NMR和13C NMR等确证结构。结论 该工艺具有原料易得、收率高、操作简便、环境友好等优点，适合工业化生产。 |
| 关键词: 雷芬那辛 路线短 合成方法 安全环保 |
| DOI： |
| 分类号:R284.1；R917.101?????? |
| 基金项目: |
|
| Research on the novel synthesis process of Revefenacin |
|
liuguomin1, shengrong2
|
|
1.Hangzhou Bio-Sincerity Pharma-Tech Co.,Ltd;2.College of Pharmaceutical Sciences, Zhejiang University
|
| Abstract: |
| OBJECTIVE Explore the improved synthetic route to Revefenacin. METHODS Revefenacin (I.) was prepared using 2-phenybenzobenzoic acid (15) and N-Boc-4-hydroxypiperidine (3) as starting material through Curtius rearrangement, nucleophilic substitution, hydrogenation and condensation. RESULTS The total yield of this synthetic route of Revefenacin was 63.4% and the structure was confirmed by HRMS, 1H NMR, and 13C NMR. CONCLUSION This synthetic route has the advantages of easily available raw materials, high yield, simple operation, and environmental friendliness, making it suitable for industrial production. |
| Key words: Revefenacin Short route synthesis method safety and environmental protection |
