伊马替尼的合成及其中间体工艺优化  

Synthesis of imatinib and the optimization of its intermediat

作　　者：罗忠枚[1] 魏玮[1] 夏小冬[1] 曹胜华[1] 丁小东[2] 

机构地区：[1]中国医药集团总公司四川抗菌素工业研究所,四川成都610052 [2]四川大学分析测试中心,四川成都610064

出　　处：《化学研究与应用》2012年第3期484-487,共4页Chemical Research and Application

摘　　要：以3-乙酰基吡啶为起始原料,经环合、缩合、还原、酰胺化等六步反应制得抗肿瘤药物伊马替尼,并对其中间体N-(2-甲基-5-硝基苯基)-4-(3-吡啶基)嘧啶-2-胺的后处理工艺进行了优化,降低了成本和操作难度,有利于工业化。The anti-cancer drug imatinib was synthesized through six main reactions such as cyclization,condensation,reduction and amidation etc.The after-treatment of N-（2-methyl-5-nitrophenyl）-4-（pyridine-3-yl）pyrimidin-2-amine,the intermediate of imatinib,was optimized greatly.The improved after-treatment method featured with low cost,easy operation procedure and could be readily scale-up to mass production.

关 键 词：3-乙酰基吡啶 伊马替尼 工艺优化 

分 类 号：O626.32[理学—有机化学]