| SB-590885的合成工艺研究 |
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| 引用本文： | 黄朋越,朱雄,赵永利,柴慧芳,赵春深.SB-590885的合成工艺研究[J].化学研究与应用,2020,32(6):1094-1099. |
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| 作者姓名： | 黄朋越 朱雄 赵永利 柴慧芳 赵春深 |
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| 作者单位： | 贵州大学化学与化工学院,贵州 贵阳 550025;贵州省合成药物工程实验室,贵州 贵阳 550025;贵州大学药学院,贵州 贵阳 55002;贵州省合成药物工程实验室,贵州 贵阳 550025;贵州中医药大学药学院,贵州 贵阳 550025;贵州省合成药物工程实验室,贵州 贵阳 550025;贵州大学药学院,贵州 贵阳 55002;贵州省合成药物工程实验室,贵州 贵阳 550025;贵州省发酵工程与生物制药重点实验室,贵州 贵阳 550025 |
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| 基金项目： | 贵州省一流大学(一期)重点建设项目;贵州省国内一流建设学科项目 |
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| 摘 要： | SB-590885是一种新型的三芳基咪唑类B-Raf激酶抑制剂,已报道的合成方法收率较低且操作繁琐,不适合工业化生产。本文设计了一条新的合成路线,以4-溴吡啶盐酸盐为起始原料,经偶联、脱保护、加成、氧化、环合、水解等反应得到目标化合物,产物结构经1H NMR,13C NMR和MS确证,总收率为9.53%,该方法原料便宜易得、反应条件温和、操作简单且总收率较高,是一条适合工业化生产的合成路线。
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| 关 键 词： | 4-溴吡啶盐酸盐 SB-590885 B-Raf激酶抑制剂 合成 |
Synthetic of SB-590885 |
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| HUANG Peng-yue,ZHU Xiong,ZHAO Yong-li,CHAI Hui-fang,ZHAO Chun-shen.Synthetic of SB-590885[J].Chemical Research and Application,2020,32(6):1094-1099. |
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| Authors: | HUANG Peng-yue ZHU Xiong ZHAO Yong-li CHAI Hui-fang ZHAO Chun-shen |
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| Institution: | (School of Chemistry and Chemical Engineering,Guizhou University,Guiyang 550025,China;School of Pharmaceutical Sciences,Guizhou University,Guiyang 550025,China;School of Pharmaceutical Sciences,Guizhou University of Traditional Chinese Medicine,Guiyang 550025,China;Guizhou Engineering Laboratory for Synthetic Drugs,Guiyang 550025,China;Key Laboratory of Guizhou for Fermentation Engineering and Biopharmacy,Guiyang 550025,China) |
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| Abstract: | SB-590885 is a new type of triarylimidazole B-Raf kinase inhibitor.The reported synthesis method has low yield and complicated operation,which is not suitable for industrial production.In this paper,a new synthetic route was designed.4-Bromopyridine hydrochloride was used as the starting material,and the target compound was obtained through coupling,deprotection,addition,oxidation,cyclization,hydrolysis and other reactions.The structure of the product was confirmed by 1H NMR,13C NMR and MS,and the total yield was 9.53%.The method had the advantages of cheap and easily available raw materials,mild reaction conditions,simple operation and high overall yield.It was a synthetic route suitable for industrial production. |
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| Keywords: | 4-bromopyridine hydrochloride SB-590885 B-Raf kinase inhibitor synthesis |
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