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.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
2011年第12期917-920,共4页
Chinese Journal of Antibiotics
关键词
抗癌药
凡德他尼
合成
Anticancer drug
Vandetanib
Synthesis