抗癌药凡德他尼的合成  

Synthesis of anticancer drug vandetanib

作　　者：刘宇[1] 夏超[1] 刘媛[1] 

机构地区：[1]南京工业大学江苏省药物研究所有限公司,南京210009

出　　处：《中国抗生素杂志》2011年第12期917-920,共4页Chinese Journal of Antibiotics

摘　　要：目的合成凡德他尼(vandetanib)并改进其合成工艺。方法以N-Boc-4-哌啶甲醇为起始原料,经磺化、缩合、N-甲基化、硝化、还原、环合、氯化、胺化反应制得凡德他尼。结果所得产物经元素分析、核磁共振谱及质谱等确证了结构。结论改进后的合成路线操作简单,收率高,易于实现工业化。Objective To synthesize vandetanib and optimize the process. Methods Vandetanib was synthesized by steps of sulfonation,condensation, N-methylation,nitrification, reduction, cyclization, chlorination and amination. Results Chemical structure of vandetanib was conformed by element analysis, 1H-NMR and ESI-MS, etc. Conclusion A more reasonable operational path for the manufacturing process of vandetanib was provided by this experiment.

关 键 词：抗癌药 凡德他尼 合成 

分 类 号：R979.1[医药卫生—药品]