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Synthetic method of avapritinib

A compound and mixed liquid technology, applied in the field of medicine, can solve problems that need to be improved, achieve good experimental operability, more reaction steps, and improve the overall yield

Active Publication Date: 2021-04-27
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 synthesizing Avapritinib still needs to be improved

Method used

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  • Synthetic method of avapritinib
  • Synthetic method of avapritinib
  • Synthetic method of avapritinib

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Embodiment Construction

[0037] 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.

[0038] Synthesis of compound shown in embodiment 1 formula 2

[0039] Compound 1 (30.0 g, 0.1 mol) was added to ethanol / water / acetic acid mixture (600 mL, preparation method: mixed ethanol, water, and acetic acid in a volume ratio of 7:3:1), heated to 70°C, Then keep dropping the mixture of L-DBTA (43.0g, 0.12mol) and ethanol / water / acetic acid (volume ratio 7:3:1, 20mL) at 70°C, and stir the resulting so...

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Abstract

The invention relates to a method for synthesizing avapritinib. Compared with the existing synthetic route, which has many reaction steps and low yield, and needs to use a chiral column to resolve chiral compounds, the method of the present invention greatly reduces the number of reaction steps, improves the total yield of the reaction, and effectively The cost of the final product is reduced, and at the same time, it has good experimental operability.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a method for synthesizing 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 metastatic GIST. In addition, ava...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04
CPCC07D487/04
Inventor 许勇范昭泽陈龙余艳平
Owner 武汉九州钰民医药科技有限公司
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