Preparation method of imatinib mesylate

A technology of imatinib mesylate and methanesulfonic acid, which is applied in the field of preparation of imatinib mesylate, can solve the problems of long reaction time, harsh reaction conditions, complicated and complicated post-processing, etc., and achieves easy operation. , The effect of reducing production cost and process optimization

Inactive Publication Date: 2020-11-20
ZHEJIANG JIANFENG PHARM CO LTD
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Problems solved by technology

This method has a long reaction time, harsh reaction conditions, complicated post-treatment, and is not suitable for industrial production.

Method used

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  • Preparation method of imatinib mesylate
  • Preparation method of imatinib mesylate

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Embodiment Construction

[0023] All features disclosed in this specification, or steps in all methods or processes disclosed, may be combined in any manner, except for mutually exclusive features and / or steps.

[0024] In this example, first use thionyl chloride to chlorinate imatinib acid [4-(4-methylpiperazin-1-ylmethyl)benzoic acid dihydrochloride] to generate imatinib mesylate Ni intermediate I; then condensed with imatinib amine [N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidinamine] to obtain imatinib mesylate The Ni intermediate II; finally with methanesulfonic acid salt to obtain imatinib mesylate. Its chemical reaction formula is as follows:

[0025]

[0026] Wherein, the preparation operation process of imatinib mesylate intermediate I [4-(4-methylpiperazine methyl) benzoyl chloride dihydrochloride] is as follows:

[0027] (1) Add 25.0kg of imatinib acid, about 300kg of thionyl chloride, and 4-7kg of DMF into a 300L replacement reaction tank, first raise the temperature to 45-70°C a...

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Abstract

The invention discloses a preparation method of imatinib mesylate. The method comprises the following steps: chlorinating imatinib acid[4-(4-methylpiperazine-1-ylmethyl)benzoic acid dihydrochloride] with thionyl chloride to generate an imatinib mesylate intermediate I; condensing the imatinib mesylate intermediate I with imatinib amine [N-(5-amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidinamine] toobtain an imatinib mesylate intermediate II, and finally salifying the imatinib mesylate intermediate II with methanesulfonic acid to obtain imatinib mesylate. According to the invention, the raw materials imatinib acid and imatinib amine used in the method are common medical intermediates, other raw materials and reagents used in the process are convenient and easy to obtain, the reaction process and post-treatment operation are simple and convenient, the yield is high, and the production cost is effectively reduced through process optimization.

Description

technical field [0001] The invention relates to a preparation method of imatinib mesylate. Background technique [0002] In the prior art, 3-nitro-4-methylaniline is used as a starting material to react with the acid chloride obtained by the acylation reaction of imatic acid chloride, and then undergoes reduction and cyanamide reaction to generate intermediate guanidine, cyclization , and finally into a salt to obtain imatinib mesylate. This method has a long reaction time, harsh reaction conditions, complicated post-treatment, and is not suitable for industrial production. The chemical reaction formula is as follows: [0003] Contents of the invention [0004] The technical problem to be solved by this invention is a kind of preparation method of imatinib mesylate, take imatinib acid as starting raw material, carry out chloroacylation reaction with thionyl chloride, obtain intermediate acyl chloride, then with Imatinib is obtained by amidation reaction of imatinib a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04
CPCC07D401/04
Inventor 蒋晓萌施存元庞雄丰理象任少波刘洋
Owner ZHEJIANG JIANFENG PHARM CO LTD
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