A practical synthesis of 4-[(4-methylpiperazin-1-yl) methyl] benzoic acid—the key precursor toward imatinib

EV Koroleva, AP Kadutskii, AV Farina, JV Ignatovich…

文献索引：Koroleva, Elena V.; Kadutskii, Aleksey P.; Farina, Alexander V.; Ignatovich, Janna V.; Ermolinskaya, Anastasiya L.; Gusak, Klaudiya N.; Kalinichenko, Elena N. Tetrahedron Letters, 2012 , vol. 53, # 38 p. 5056 - 5058

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被引用次数: 8

摘要

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 ...