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Method for preparing targeted anti-cancer drug avapritinib

A compound and solution technology, applied in the field of medicine, can solve problems that need to be improved, and achieve the effects of good experimental operability, increased yield, increased selectivity and total yield

Inactive Publication Date: 2020-04-03
武汉九州钰民医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The current method of preparing Avapritinib still needs to be improved

Method used

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  • Method for preparing targeted anti-cancer drug avapritinib
  • Method for preparing targeted anti-cancer drug avapritinib
  • Method for preparing targeted anti-cancer drug avapritinib

Examples

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Embodiment Construction

[0038] Embodiments of the present invention are described in detail below. The embodiments described below are exemplary only for explaining the present invention and should not be construed as limiting the present invention. If no specific technique or condition is indicated in the examples, it shall be carried out according to the technique or condition described in the literature in this field or according to the product specification. The reagents or instruments used were not indicated by the manufacturer, and they were all commercially available conventional products.

[0039] Synthesis of compound shown in embodiment 1 formula 2

[0040] At 0°C, compound 1 (30.1 g, 0.1 mol) was added to DCM (25 mL), stirred, and saturated NaHCO was added 3 solution (120mL), then slowly added dropwise (Boc) 2 O (24.0g, 0.11mol), kept stirring at 25°C for 3h. The organic layer was separated, the aqueous phase was extracted with DCM solution (300 mL), and the organic phases were combine...

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Abstract

The invention relates to a method for preparing targeted anti-cancer drug avapritinib. According to the route, the intermediate which is easy to obtain at present is used as a starting raw material, Boc protection is performed on amino, and then the halogenation reaction is performed, so that the yield of the halogenation reaction is effectively improved, and halogenation byproducts on imine are prevented from being generated.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a method for preparing the targeted anticancer drug avapritinib. Background technique [0002] Avapritinib (BLU-285) is a small molecule kinase inhibitor that can effectively inhibit the activity of PDGFRα D842V mutant; it is also an inhibitor of KIT mutation (KIT D816V). Avapritinib selectively and potently inhibits KIT and PDGFRA mutant kinases. Avapritinib has demonstrated broad inhibitory activity against gastrointestinal stromal tumor (GIST)-associated KIT and PDGFRA mutations, including robust activity against activating loop mutations associated with resistance to currently approved therapies. Compared with approved multikinase inhibitors, avapritinib is significantly more selective for KIT and PDGFRA than other kinases. Avapritinib has been granted breakthrough drug designation by the FDA for the treatment of patients with PDGFRαD842V mutation, unresectable or metastat...

Claims

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Application Information

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IPC IPC(8): C07D487/04
CPCC07D487/04
Inventor 许勇余艳平范昭泽陈龙
Owner 武汉九州钰民医药科技有限公司
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