| Flavopiridol合成工艺的改进 |
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| 引用本文： | 李艳玲,方浩,徐文方.Flavopiridol合成工艺的改进[J].包头医学院学报,2009,25(2):119-121. |
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| 作者姓名： | 李艳玲 方浩 徐文方 |
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| 作者单位： | 包头医学院药学系,内蒙古,包头,014060;山东大学药学院;山东大学药学院 |
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| 基金项目： | 国家高技术研究发展计划(863计划) |
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| 摘 要： | 目的：改进Flavopiridol的合成工艺。方法：以1-甲基-4-（2，4，6-三甲氧基）-1，2，3，6-四氢吡啶为原料，利用Dalton反应制得环氧，而后经A1H3还原制得Flavopiridol的关键中间体3-哌啶醇，后经拆分、酰化、选择性脱甲基、羟醛缩合、查尔酮氧化关环、脱甲基制得Flavopiridol。结果：目标化合物经^1 H—NMR、质谱确证；总收率为11．8％，比文献报道的收率提高4．8％。结论：改进后的方法不仅条件温和、反应的立体选择性大为提高，而且操作简单。
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| 关 键 词： | Dalton反应 AlH3还原 查尔酮路线 |
Improvement in Synthetic Technology of Flavopiridol |
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| LI Yanling,FANG Hao,XU Wenfang.Improvement in Synthetic Technology of Flavopiridol[J].Journal of Baotou Medical College,2009,25(2):119-121. |
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| Authors: | LI Yanling FANG Hao XU Wenfang |
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| Institution: | LI Yanling1,2,FANG Hao2,XU Wenfang2(1.Department of Pharmacy,Baotou Medical College,Baotou 014000,China,2.School of Pharmacy,Sh,ong University) |
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| Abstract: | Objective: To improve the synthetic technology of flavopiridol.Methods: Dalton reaction was employed to produce the synthesis of expoxide from 1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydropyridine,then key intermediate of flavopiridol-piperidol was got by means of AlH3 reduction of expoxide.finally,flavopiridol was prepared via acylation,selective demethylation,adol consendation,chalcone closure,demethylation.Results: The structure of target compound was confirmed by 1H-NMR,MS and the overall yield... |
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| Keywords: | Dalton reaction AlH3 reduction Chalcone route |
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