瑞格拉非尼的合成  

Synthesis of regorafenib

作　　者：王亚博[1] 尚伟定 包依凡 石晓伟[1] 杜玉民[1] 曹德英[1] 张恺[1] 

机构地区：[1]河北医科大学药学院,石家庄050017 [2]中国药科大学药学院,南京211100

出　　处：《中国抗生素杂志》2015年第8期590-592,共3页Chinese Journal of Antibiotics

基　　金：河北省科技支撑计划项目(No.13272603D);河北省高等学校科学研究优秀青年基金项目(No.YQ2014031)

摘　　要：目的合成新型多激酶抑制剂类抗癌药物瑞格拉非尼。方法以对氨基苯磺酸为起始原料,经重氮化、偶合、还原、亲核取代及CDI缩合反应得目标化合物。结果目标化合物经1H-NMR、MS确证结构,总收率52.6%。结论该制备过程操作简便,收率高,为中试生产提供了依据。Objective To synthesize regorafenib, a novel anticancer drug with multi-kinase inhibition. MethodsStarting from sulfanilic acid, regorafenib was prepared successively via diazotization, coupling reaction, reduction,nucleophilic substitution and CDI condensation. Results The target compound was successhlly obtained with a totalyield of 52.6%, and its chemical structure was confirmed by 1H-NMR and MS spectra. Conclusion This simple andhigh yielding process should lay foundation for pilot-scale production.

关 键 词：瑞格拉非尼 抗癌药物 合成 

分 类 号：R9[医药卫生—药学]