吡莫地韦的合成工艺研究  

Study on the syntheticprocesss of pimodivir

作　　者：刘呈武 李波 周光强 蔡泽绵 黎志豪 LIU Chengwu;LI Bo;ZHOU Guangqiang;CAI Zemian;LI Zhihao(Technology Development Department,Guangdong Zhongsheng Raynovent Biotechnology Co.,Ltd.,Guangzhou 510700,China)

机构地区：[1]广东众生睿创生物科技有限公司工艺开发部,广东广州510700

出　　处：《中国药物化学杂志》2025年第1期34-38,共5页Chinese Journal of Medicinal Chemistry

摘　　要：目的优化吡莫地韦的合成工艺。方法以2-氨基-5-氟吡啶(2)为起始原料,经碘代、偶联、环合、溴代、磺酰化、硼酸酯化、偶联、水解和脱除保护基得到吡莫地韦。结果目标化合物吡莫地韦的结构经^(1)H-NMR、^(13)C-NMR和ESI-MS谱确证,总收率为43.9%(以化合物2计),纯度为99.5%(HPLC)。结论通过优化反应条件和后处理方法,使吡莫地韦的合成工艺操作简便,避免使用柱色谱分离纯化,提高了总收率,有利于大量制备。An improved synthetic process of pimodivir was reported.2-Amino-5-fluoropyridine(2)was used as starting materials.The targeted compound was afforded by iodination,coupling,ring closure,bromination,tosylation,boration,coupling,hydrolysis and deprotection.The structure of pimodivir was confirmed by^(1)H-NMR,^(13)C-NMR and ESI-MS.The overall yield was up to 43.9%(based on compound 2)with the purity of 99.5%(HPLC).By optimizing the reaction conditions and post-processing methods,the synthetic process of pimodivir can be made simple and avoid the use of column chromatography for purification,which improves the overall yield and makes it possible to produce in large quantities.

关 键 词：吡莫地韦 流感病毒聚合酶抑制剂 工艺优化 

分 类 号：R914[医药卫生—药物化学]