Author/Authors :
Koroleva، نويسنده , , Elena V. and Kadutskii، نويسنده , , Aleksey P. and Farina، نويسنده , , Alexander V. and Ignatovich، نويسنده , , Janna V. and Ermolinskaya، نويسنده , , Anastasiya L. and Gusak، نويسنده , , Klaudiya N. and Kalinichenko، نويسنده , , Elena N.، نويسنده ,
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.
