凡德他尼的合成路线图解  

Graphical Synthetic Routes of Vandetanib

作　　者：王敏[1] 王文惠[1] 朱五福[1] 

机构地区：[1]江西科技师范大学药学院,江西南昌330013

出　　处：《精细化工中间体》2015年第4期9-12,共4页Fine Chemical Intermediates

摘　　要：通过总结已有的凡德他尼的合成方法,对不同的合成路线进行分析,提出适合工业化生产的合成路线。以N-Boc-4-对甲苯磺酰基氧甲基哌啶(6)和香草酸乙酯(22)为原料经取代、去保护、甲基化、硝化还原、环合、氯代、取代合成目标化合物1。该工艺相对简单,成本较低,收率较高,具有工业化生产前景。To review the existing synthetic routes of vandetanib was summarized, and different synthetic routes were analyzed to find a suitable industrial production of synthetic routes. By analyzing and summarizing these synthetic route discovery that tea-butyl 4-（（tosyloxy）methyl）piperidine-1-carboxylate（6） and ethyl vanillate （22） were subjected to substitution, deprotection, methylation, nitration, reduction, cyclization, chlorination, substitution to give the title compound （1）. It showed more favorable, yield higher and commercial value in the manufacturing scale.

关 键 词：凡德他尼 酪氨酸酶抑制剂 合成路线图解 

分 类 号：R914.5[医药卫生—药物化学]