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Method for synthesizing and preparing anti-tumor innovative drug, namely Devimistat

A compound and sodium hydroxide technology, applied in the field of medicine, can solve problems such as the need for improvement of Devimistat, and achieve the effects of high utilization rate, high yield and high purity of reactants

Inactive Publication Date: 2020-07-03
武汉九州钰民医药科技有限公司
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Problems solved by technology

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

Method used

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  • Method for synthesizing and preparing anti-tumor innovative drug, namely Devimistat
  • Method for synthesizing and preparing anti-tumor innovative drug, namely Devimistat
  • Method for synthesizing and preparing anti-tumor innovative drug, namely Devimistat

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Embodiment Construction

[0025] 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.

[0026] Synthesis of compound shown in embodiment 1 formula I

[0027] Compound 1 (1.0 g, 4.85 mmol) was added into 0.5 M sodium hydroxide (10 mL), stirred at room temperature until completely dissolved. Then heated to 40°C, then added sodium borohydride (183.4mg, 4.85mmol), stirred for 1h, TLC or HPLC detected that the reaction solution was completely reacted, and the reaction solution containing compoun...

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Abstract

The invention relates to a method for synthesizing and preparing an anti-tumor innovative drug, namely Devimidat. According to the preparation method for the Devimidat, after a process is improved, metal cobalt polysulfide does not need to be used any more; the process route is simple and convenient; the product, namely the Devimidat can be obtained through two steps which are performed through aone-pot method; and the preparation method has high yield and is applicable to large-scale production.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a method for synthesizing and preparing an innovative anti-tumor drug Devimistat. Background technique [0002] Devimistat (CPI-613) is an innovative anti-tumor drug developed by Rafael Pharmaceuticals. Its current highest research and development status is Phase 3. Its clinical research in the United States, Europe, South Korea, Israel, etc. is used for the treatment of acute myeloid leukemia , and metastatic pancreatic cancer, its indications for Burkitts lymphoma and cholangiocarcinoma are currently in phase 2 clinical studies. Devimistat is a lipoic acid analog that inhibits pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts mitochondrial metabolism and exhibits potent antitumor activity. In the United States, in July 2008, Devimistat was granted orphan drug qualification for the treatment of pancreatic cancer by the FDA; in September 2011, it was gran...

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Application Information

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IPC IPC(8): C07C319/14C07C323/52
CPCC07C319/06C07C319/14C07C323/52
Inventor 许勇范昭泽余艳平
Owner 武汉九州钰民医药科技有限公司
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