Chemagis Ltd.

Liu Xing

Lei Zhang

Joseph Kaspi

Sonia Krivonos

Edna Danon

Lior Zelikovitch

He Xungui

Michel Bekhazi

Huang Anli

Provided is a process for producing imatinib and salts thereof, e.g., imatinib mesylate. The process includes reacting 4-(4-methyl-piperazin-1-ylmethyl)-benzoic acid with N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidine-amine in the presence of a carboxylic acid coupling reagent, to produce imatinib, and optionally converting the imatinib into a salt.

Imatinib production process

A novel process is disclosed for producing Imatinib, using the precursor 2-chloro-4-(3-pyridyl)-pyrimidine, thus improving Imatinib preparation via an alternative synthetic route, avoiding the use of the toxic reagent cyanamide.

Process for preparing Imatinib

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Shanghai, China

Liu Xing