Improved synthesis of imatinib mesylate / 药学实践杂志

ABSTRACT

Objective To obtain the improved synthesis of imatinib mesylate .Methods 4-[(4-methyl-piperazin-1-yl) methyl〗benzoyl chloride dihydrochloride and 4-methyl-N3-[4-(3-pyridyl) pyrimidin-2-yl]-1,3-phenylenediamine were used as starting raw mate-rial to perform a condensation reaction in the aqueous phase to give imatinib free base , which was then neutralized with methanesulfonic acid to obtain the novel antineoplastic tyrosinase inhibitor imatinib mesylate by the use of a two -step reaction .Results The improved syn-thesis was considered to have the advantages of low cost , easy post-processing, high purity, high yield and environmental pollution with the HPLC purity≥99.7%and the single impurity<0.1%.Conclusion The total yield of the novel method was 81.5%, having an e-nough broad industrial production prospect .The targeted compound structure was confirmed by 1 H NMR and ESI-MS.