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Preparation method of medicine for treating fascioliasis

A compound, room temperature technology, applied in the field of medicine, can solve the problems such as the preparation method of Triclabendazole needs to be improved, and achieve the effects of improving the total yield and operability, the separation is simple, and the number of reaction steps is small.

Inactive Publication Date: 2020-04-28
武汉九州钰民医药科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The preparation method of Triclabendazole still needs to be improved at present

Method used

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  • Preparation method of medicine for treating fascioliasis
  • Preparation method of medicine for treating fascioliasis
  • Preparation method of medicine for treating fascioliasis

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Embodiment Construction

[0039] 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.

[0040] Synthesis of compound shown in embodiment 1 formula 3

[0041] At 0°C, compound 1 (15.9 g, 0.1 mol), compound 2 (9.13 g, 0.12 mol), Na 2 CO 3 (7.42g, 0.07mol), heated to reflux for 5h. The reaction solution was cooled to room temperature, suction filtered, and dried to obtain the compound shown in formula 3. The yield was 18.6 g, and the yield was 92.7%. The compound shown in formula 3 was direc...

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PUM

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Abstract

The invention provides a preparation method of Triclabendazole, and relates to a preparation method of Triclabendazole. Compared with the existing synthetic route with many and complex reaction steps,the preparation method provided by the invention has the advantages that the reaction steps are few, the separation is simple and convenient, and the total yield and operability of the reaction are improved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of a medicine for treating fascioliasis. Background technique [0002] Fascioliasis, also known as liver fluke infection, is a neglected tropical disease. Worldwide, approximately 2.4 million people are affected, with another 180 million people at risk. [0003] On February 13, 2019, the FDA approved Novartis's Triclabendazole (Triclabendazole, also known as Triclobenazole) for marketing. The specification dosage form is: 250mg tablet, trade name: Egaten, clinically used to treat children over 6 years old. Patients with fascioliasis. Egaten is currently the only therapy recommended by the World Health Organization (WHO) for the treatment of fascioliasis, and it is one of the drugs on the WHO Model List of Essential Medicines. [0004] The structural formula of Triclabendazole is the compound shown in formula I: [0005] [0006] At present, the prepar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D235/28A61P33/12
CPCA61P33/12C07D235/28
Inventor 许勇范昭泽陈龙顿伟
Owner 武汉九州钰民医药科技有限公司