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RET inhibitor and preparation method thereof

A technology of mixing solvents and compounds, which is applied in the field of medicine, can solve the problems that the preparation method of Selpercatinib needs to be improved, and achieve the effects of good economic advantages, increased total yield, and high utilization rate

Active Publication Date: 2020-04-24
武汉九州钰民医药科技有限公司
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

[0007] At present, the research on the RET inhibitor Selpercatinib still needs to be in-depth, and the preparation method of Selpercatinib still needs to be improved

Method used

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  • RET inhibitor and preparation method thereof
  • RET inhibitor and preparation method thereof
  • RET inhibitor and preparation method thereof

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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 3

[0039] At 0° C., NaH (2.64 g, 0.11 mol) was added in portions to compound 1 (25.4 g, 0.1 mol) in DMF (240 mL), and the reaction was kept at 0° C. and stirred for 15 min after the addition was complete. Then compound 2 (72 g, 1 mol) was added to the reaction liquid at 25 °C, and after the addition was completed, the temperature was raised to 8...

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Abstract

The invention relates to an RET inhibitor and a preparation method thereof. The preparation method provided by the invention has the advantages of fewer reaction steps and mild reaction conditions, sothat the total yield of the reaction product is greatly improved, the product purity reaches 99.5% or above, and the preparation method has good economic advantages.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to a RET inhibitor and a preparation method thereof. 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 gene f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D519/00A61P35/00
CPCA61P35/00C07D519/00
Inventor 许勇陈龙范昭泽余艳平
Owner 武汉九州钰民医药科技有限公司
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