A simple and efficient in situ synthesis of 4-[(4-methylpiperazin-1-yl)methyl]benzoic acid through direct reductive alkylation of 1-methylpiperazine in the presence of triacetoxy sodium borohydride in 95–99% yields is elaborated. The process is easy to scale-up for the large-scale synthesis of 4-[(4-methylpiperazin-1-yl)methyl]benzoic acid as the key synthetic intermediate of imatinib. This method was used for the synthesis of benzyl derivatives of heterocyclic amines in 87–90% yields.

中文翻译：

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实用合成4-[（（4-甲基哌嗪-1-基）甲基]苯甲酸-伊马替尼的关键前体

阐述了在三乙酰氧基硼氢化钠存在下，通过1-甲基哌嗪的直接还原烷基化，简单有效地原位合成4-[（4-甲基哌嗪-1-基）甲基]苯甲酸的产率为95-99％。该方法易于规模化，可大规模合成4-[（4-甲基哌嗪-1-基）甲基]苯甲酸作为伊马替尼的关键合成中间体。该方法用于合成杂环胺的苄基衍生物，产率为87–90％。