A new method for imatinib synthesis is described by using the C–N coupling reaction of 4-(4-methylpiperazine-1-methyl)benzamide with N-(5-bromo-2-tolyl)-4-(3-pyridyl)pyrimidin-2-amine to form imatinib. In this synthetic route, the high efficiency and high selectivity of nano-ZnO as a catalyst is key to the mild hydrolysis of 4-(4-methylpiperazine-1-methyl)benzonitrile into the corresponding amide. The total imatinib yield was 51.3%, and the purity was 99.9%. This simple and effective synthetic pathway avoids gene-impurity production (as classified by the FDA Center for Drug Evaluation and Research), and the synthesis is environmentally friendly with a short reaction time.

中文翻译：

---

伯酰胺与溴取代的嘧啶胺的CN偶联反应合成伊马替尼

通过使用4-（4-甲基哌嗪-1-甲基）苯甲酰胺与N-（5-溴-2-甲苯基）-4-（3-吡啶基）嘧啶的C–N偶联反应描述了一种合成伊马替尼的新方法-2-胺形成伊马替尼。在这种合成路线中，纳米ZnO作为催化剂的高效率和高选择性是将4-（4-甲基哌嗪-1-甲基）苄腈温和水解为相应酰胺的关键。伊马替尼的总产率为51.3％，纯度为99.9％。这种简单有效的合成途径避免了基因杂质的产生（由FDA药物评估和研究中心分类），并且该合成对环境友好，反应时间短。