Method for preparing alpha-imatinib mesylate

Abstract

The invention discloses a method for preparing alpha-imatinib mesylate, and belongs to the field of medicines. The method comprises the following steps of: suspending imatinib base in a mixed solvent of water and an organic solvent, stirring, and adjusting the temperature to be 20-30DEG C; dissolving methanesulfonic acid, and dripping into reaction liquid; after the dripping is finished, standingfor clarifying the liquid, heating to the temperature of between 50 and 60DEG C, and keeping the temperature to react for 0.5 to 1 hour; and reducing the temperature to 32-40DEG C, adding alpha-imatinib mesylate seed crystals, dripping the organic solvent, continuously reducing the temperature to 20-30DEG C, separating out crystals, filtering, and drying to obtain a product. The preparation method has the advantages of simple operation, short reaction time, high yield, high purity of alpha-imatinib mesylate, low production cost, and suitability for industrial production.

Description

A method for preparing α-type imatinib mesylate technical field The invention relates to a method for preparing α-type imatinib mesylate, which belongs to the field of medicine. Background technique Imatinib Mesylate is a tyrosine kinase inhibitor drug developed by Novartis, Switzerland. Chinese chemical name: 4-[(4-Methyl-1-piperazine)methyl]-N-[4-methyl-3-[[4-(3-pyridine)-2-pyrimidine]amino]phenyl]-Benzene Amide methanesulfonate English chemical name: 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide, Methanesulfonate Chemical structure: In May 2001, imatinib mesylate was approved by the U.S. FDA for its breakthrough anti-tumor mechanism. For the treatment of myeloid leukemia (CML, Chronic Myebginous Leukemia), the trade name is Glivec; in February 2002, the US FDA approved this product for the treatment of gastrointestinal stromal cell tumors. There are currently 10 FDA-approved indications for imatinib....

AI Technical Summary

Problems solved by technology

Because the melting point of α-type imatinib mesylate prepared by method (1) is on the low side, and a small amount of β-type products also exist in the α-type imatinib mesylate prepared by method (2), although method (3) The above situation has been improved, but the price of various ketones used in the preparation process is higher, resulting in higher costs in the production process

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