E. V. Koroleva, Aleksey P. Kadutskii, A. Farina
Sep 19, 2012
Citations
0
Influential Citations
11
Citations
Journal
Tetrahedron Letters
Abstract
Abstract 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.