【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AlH3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1H-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。更多还原

【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 was 11.8%.Compared with that reported in the literature,the overall yield was increased by 4.8%.Conclusion: This synthetic process is suitable for the preparation of multigram quantities by its convenient operation,mild reaction conditions and higher stereoselectivity.This method has not been reported at home.更多还原