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Preparation method of cabozantinib

A technology of cabozantinib and dichloromethane, applied in the field of preparation of cabozantinib, can solve problems such as equipment corrosion and serious environmental pollution, and achieve the effects of convenient post-processing, improved reaction yield, and convenient operation

Inactive Publication Date: 2018-07-10
南京法恩化学有限公司
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  • Abstract
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  • Claims
  • Application Information

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Problems solved by technology

The main disadvantage of this method is that a large amount of highly poisonous phosphorus oxychloride, sulfur dioxide and oxalyl chloride are used, which causes serious environmental pollution and serious corrosion of equipment.

Method used

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  • Preparation method of cabozantinib

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Embodiment Construction

[0023] The technical solutions in the present invention are clearly and completely described below in conjunction with the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without making creative efforts belong to the protection scope of the present invention.

[0024] The present embodiment provides a kind of preparation method of cabozantinib, such as figure 1 As shown, it specifically includes the following steps:

[0025] Step 1: Add 1L of dichloromethane into the reaction flask, add 150g of 6,7-dimethoxy-4-hydroxyquinoline and 100g of triethylamine, add 150g of p-toluenesulfonyl chloride and 100ml of di Chloromethane solution. After the reaction was completed, the liquid was separated, and the dichloromethane layer was washed with sodium bicarbonate solution, concentrated, crystallized, filtered, and dried to obtain 260 g of intermediate 1 with a yield of 99%.

[0026] Step 2: Add 1L ...

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Abstract

The invention relates to a preparation method of cabozantinib. The method comprises the following steps: taking 5,6-dimethoxy-4-hydroxyquinoline, TsCl, fluoronitrobenzene, and 1-(4-fluorophenyl)amino-carbonyl cyclopropane carboxylic acid as raw materials, and performing steps of a hydroxy protection reaction, a coupling reaction, a reduction reaction, and a condensation reaction to obtain the cabozantinib. The preparation method of cabozantinib has the advantages of high yield, low cost, less three wastes, easy operation, and safety, and is suitable for industrialization.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a preparation method of cabozantinib. Background technique [0002] Cabozantinib is a new type of multi-target tyrosine kinase inhibitor developed by Exelixis Biopharmaceutical Company of the United States. As a tyrosine kinase inhibitor that inhibits MET, vascular endothelial growth factor receptor 2 (VEGFR2) and RET, it can block the occurrence and development of tumor cells, and is clinically used for progressive and metastatic medullary thyroid carcinoma (MTC) ) treatment of patients. On November 19, 2012, it was approved by the US FDA for the treatment of unresectable malignant locally advanced or metastatic medullary thyroid carcinoma (MTC). Cabozantinib (cabozantinib, XL184, BMS-907351) is the second drug approved for the treatment of medullary thyroid cancer in the past 2 years, and the other drug is Caprelsa from AstraZeneca. Medullary thyroid carcinoma (MTC) is a rare, refra...

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Application Information

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IPC IPC(8): C07D215/22
CPCC07D215/22
Inventor 王坤鹏韩月林
Owner 南京法恩化学有限公司
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