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

作　　者：童航 詹一丰 何世波 王溥照 刘明星 TONG Hang;ZHAN Yi-feng;HE Shi-bo;WANG Pu-zhao;LIU Ming-xing(School of Biological Engineering and Food,Hubei University of Technology,Wuhan 430068,China)

机构地区：[1]湖北工业大学生物工程与食品学院,湖北武汉430068

出　　处：《化学研究与应用》2022年第5期1229-1232,共4页Chemical Research and Application

基　　金：国家级大学生创新创业训练计划项目(202010500019)资助。

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、^(1)H NMR、^(13)C 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。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,^(1)HNMR and ^(13)CNMR.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.

关 键 词：培西达替尼 培西达替尼中间体 抗癌药物 合成 

分 类 号：O626.32[理学—有机化学]