A practical synthesis of 4-[(4-methylpiperazin-1-yl)methyl]benzoic acid—the key precursor toward imatinib
2012
Koroleva, Elena V. | Kadutskii, Aleksey P. | Farina, Alexander V. | Ignatovich, Janna V. | Ermolinskaya, Anastasiya L. | Gusak, Klaudiya N. | Kalinichenko, Elena N.
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.
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