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Preparation method of albendazole

A technology of albendazole and compounds, which is applied in the field of preparation of new albendazole, can solve the problems of low total yield and great harm to human body, and achieve the effects of simple operation, small damage and cost reduction

Active Publication Date: 2011-11-23
湖南欧亚药业有限公司
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Problems solved by technology

[0010] The first method and the second method have many steps, and the total yield is low; although the third method has few steps, it uses chlorosulfonic acid which is volatile and harmful to the human body as a raw material

Method used

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  • Preparation method of albendazole
  • Preparation method of albendazole
  • Preparation method of albendazole

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Embodiment Construction

[0022] In order to make the technical means, creative features, work flow, and use methods of the present invention achieve the purpose and effect easily understood, the present invention will be further described below in conjunction with specific embodiments.

[0023] The chemical reaction equation of the present invention is as follows:

[0024]

[0025] Synthesis of compound II:

[0026] Add 382 grams to the reaction bottle (I) (2.0mol), 261.8 grams of potassium bromide (2.0mol), 11.7 grams of ammonium metavanadate and 1200 milliliters of chloroform, under stirring, the temperature was raised to 40-45 ° C, and 907 grams of 30% hydrogen peroxide (8.0mol ), the dropwise addition was completed, and the reaction was continued at this temperature for 2 hours, then the temperature was raised to 75°C, and the reaction was continued for 30 minutes. After the reaction was completed, it was cooled to room temperature, and the reaction layers were separated. The aqueous layer wa...

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Abstract

The invention discloses a preparation method of albendazole. In the method, a compound as shown in a formula (I) is used as a raw material, and albendazole is obtained through two steps of bromination and substitution. The preparation method has the advantages of less steps, cheap and available raw material, little pollution and high yield, is simple to operate and is suitable for industrial production.

Description

technical field [0001] The present invention relates to a kind of preparation method of novel albendazole. Background technique [0002] Albendazole (Albenzadole), also known as albendazole, chemically named 5-propylthio-1H-benzimidazole-2-carbamate methyl ester, is a spectrally efficient and low-toxic anthelmintic drug. The drug is produced by the United States. Smith Kline was first listed in the market in 1977, and it is widely used clinically in various helminth infectious diseases. Its mechanism of action is mainly to inhibit the fumarate reductase of the worm body, prevent the energy generation of the worm body, and thus achieve the purpose of killing the worm body. The drug has a strong killing effect on human and animal parasitic nematodes, trematodes and tapeworms, and can significantly inhibit the development of eggs, and has no accumulation in the body. Other helminth drugs, the drug has now been included in the medical insurance products, and has become the firs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D235/32
Inventor 林开朝李兴民陶友妮
Owner 湖南欧亚药业有限公司
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