Method for preparing RET inhibitor Selpercatinib

A technology of inhibitors and compounds, applied in the field of medicine, can solve problems that need to be improved, and achieve the effect of high utilization rate, high risk and high purity of reactants

Active Publication Date: 2020-04-14
武汉九州钰民医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] The current method for preparing the RET inhibitor Selpercatinib still needs to be improved

Method used

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  • Method for preparing RET inhibitor Selpercatinib
  • Method for preparing RET inhibitor Selpercatinib
  • Method for preparing RET inhibitor Selpercatinib

Examples

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Embodiment Construction

[0032] 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.

[0033] Synthesis of compound shown in embodiment 1 formula 3

[0034] In acetone (300mL), add compound 1 (33.2g, 0.1mol), compound 2 (18.4g, 0.12mol), K 2 CO 3 (16.6g, 0.12mol) and tetrabutylammonium bromide (3.2g, 0.01mol), stirred and heated, and reacted under reflux at 60°C for 12h. After the reaction solution was filtered, the filtrate was concentrated, and the obtained solid was purified by beatin...

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Abstract

The invention relates to a method for preparing an RET inhibitor Selpercatinib. The preparation method provided by the invention has the advantages of mild halogenation reaction conditions, simple andconvenient reaction operation steps and post-treatment and few reaction steps, has the substantially increased total yield of the reaction, and achieves the product purity of more than 99.0%.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a method for preparing the RET inhibitor Selpercatinib. Background technique [0002] RET is a proto-oncogene (transfection rearranged gene, The REarranged during Transfection). RET receptor tyrosine kinase is an oncogene that appears in various cancers including non-small cell lung cancer (NSCLC) and medullary thyroid carcinoma (MTC), and its abnormal activation is a key driver for the growth and proliferation of various solid tumors It has been found that the occurrence of many diseases is closely related to RET gene mutations, such as NSCLC, MTC, multiple endocrine neoplasia type Ⅱ (MEN2), papillary thyroid carcinoma (papillary thyroidcarcinomas, PTC), Hirschsprung disease, lung adenocarcinoma, etc. [0003] RET gene variants include gene fusions and activating point mutations, which can lead to overactivation of the RET signaling pathway and uncontrolled cell growth. RET ...

Claims

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Application Information

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IPC IPC(8): C07D519/00
CPCC07D519/00
Inventor 许勇余艳平陈龙范昭泽
Owner 武汉九州钰民医药科技有限公司
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