索拉非尼的合成  

Synthesis of Sorafenib

作　　者：孙敏[1] 魏红涛[1] 蔡进[1,2] 吉民[1,2] 

机构地区：[1]东南大学化学化工学院制药工程系,南京210096 [2]东南大学制药工程研究所,南京210096

出　　处：《中国药学杂志》2009年第5期394-396,共3页Chinese Pharmaceutical Journal

摘　　要：目的合成抗肿瘤新药索拉非尼。方法以2-吡啶甲酸(2)为原料,经卤化,酰胺化,成醚制得中间体(6),再和4-氯-3-(三氟甲基)苯胺(7)成脲制得索拉非尼(1)。结果以总收率56%合成了索拉非尼,结构经核磁氢谱(1H-NMR)、质谱(MS)确证。结论本方法原料易得,操作简单,总收率较高,而且整个过程不需柱色谱纯化,适合工业化生产。OBJECTIVE To synthesize sorafenib a new anti-tumor drug .METHODS The intermediate was obtained by halogenation, amidation and etherification with picolinic acid （2） as the starting compound. Sorafenib was obtained by ureas formation. RESULTS The total yield was 56%. The structure was verified by 1H-NMR and MS. CONCLUSION The route is effective, simple and highly productive, and there was no need to use column chromatography in all preparation steps. The process may be suitable for industrial applications.

关 键 词：索拉非尼 多激酶抑制剂 合成 

分 类 号：R914.5[医药卫生—药物化学]