Preparation method of imatinib

Abstract

The invention discloses a preparation method of imatinib, wherein the needed component imatinib is finally generated through conversion of an intermediate. According to the preparation method of the imatinib disclosed by the invention, the synthetic steps are fewer, the raw materials adopted are cheap and easy to obtain, the environment is less polluted, and the yield is high, so that the preparation method of the imatinib is appropriate for industrial production.

Description

technical field [0001] The invention relates to the field of pharmaceutical chemical synthesis, in particular to a preparation method of Imatinib. Background technique [0002] Imatinib Mesilate (Imatinib Mesilate) is a signal transduction inhibitor (formerly STI571) successfully developed by Norvatis, Switzerland after 7 years of research. It is the first approved tumorigenesis-related signal transduction in the world. Inhibitor for the treatment of patients with chronic myelogenous leukemia in the blast crisis, accelerated or chronic stages of alpha-interferon (interfer on-alfa) therapy. Imatinib mesylate has obtained the status of an orphan drug in the United States, Europe, Japan and other countries, and was approved by the US FDA on May 10, 2001. [0003] The chemical name of Imatinib is: 4-(4-methylpiperazinyl-1-methyl)-N-{4-methyl-3-[4-(3-pyridyl)pyrimidinyl) -2-amino]} benzamide, the structural formula is as follows: [0004] [0005] Imatinib [0006] There h...

AI Technical Summary

Problems solved by technology

[0021] This route is used in the synthesis of important intermediates In the process, on the one hand, a highly toxic and low-boiling methyl iodide reagent is used; on the other hand, the intermediate is a sulfide compound, which has a foul smell and is relatively harmful to the environment.

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