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6-({[6-(三氟甲基)吡啶-3-基]甲基}氨基)吡啶-3-甲醛的合成
Synthesis of 6-({[6-(trifluoromethyl)pyridin-3-yl]methyl}amino) pyridine-3-carbaldehyde
【摘要】 6-({[6-(三氟甲基)吡啶-3-基]甲基}氨基)吡啶-3-甲醛是抗癌药物培西达替尼的关键中间体。本文以6-氨基烟酸甲酯和6-三氟甲基烟醛为原料,经还原胺化、还原和氧化共三步反应合成目标化合物,产物结构经MS、IR、1H NMR、13C NMR分析表征;同时探讨了不同条件对反应的影响。在最佳工艺条件下,产物总产率达58.6%。该合成路线具有原料廉价易得、条件温和、操作简便等优点,可望实现规模化生产。
【Abstract】 6-({[6-(Trifluoromethyl)pyridin-3-yl]methyl}amino)pyridine-3-carbaldehyde is used as the key intermediate of the anticancer drug pexidartinib.In this article, the title compound was synthesized from methyl 6-aminonicotinate and 6-(trifluoromethyl)nicotinaldehyde through three steps of reductive amination reaction, reduction reaction and oxidation reaction.The product was characterized by MS,IR,1HNMR and 13CNMR.At the same time, the influence of different conditions on the reaction was also discussed.Under the best technological conditions, the total yield of the product reached 58.6%.The synthetic route had the advantages of cheap raw materials, mild conditions and simple operation, which could realize large-scale production.
【Key words】 pexidartinib; intermediate of pexidartinib; anti-cancer drugs; synthesis;
- 【文献出处】 化学研究与应用 ,Chemical Research and Application , 编辑部邮箱 ,2022年05期
- 【分类号】TQ463.5
- 【下载频次】56