Title of article
A practical synthesis of 4-[(4-methylpiperazin-1-yl)methyl]benzoic acid—the key precursor toward imatinib
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 ,
Issue Information
هفته نامه با شماره پیاپی سال 2012
Pages
3
From page
5056
To page
5058
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.
Keywords
Benzyl derivatives , reductive alkylation , Imatinib
Journal title
Tetrahedron Letters
Serial Year
2012
Journal title
Tetrahedron Letters
Record number
1881940
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