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Method for synthesizing pasiniazide

A technology of isoniazid p-aminosalicylate and p-aminosalicylic acid, which is applied in the field of compound preparation, can solve problems such as metabolic inactivation of acetylated compounds, and achieve the effects of high product yield, good product quality and low cost

Inactive Publication Date: 2005-01-12
张之君
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Isoniazid has inhibitory and killing effects on Mycobacterium tuberculosis, but isoniazid can generate acetylated substances in the body to be metabolically inactivated

Method used

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  • Method for synthesizing pasiniazide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Put 15 kg of isoniazid in a reaction tank, add 200 kg of absolute ethanol, heat to 50° C. and stir. After the isoniazid is completely dissolved, add 16.75 kg of p-aminosalicylic acid. Continue stirring at the same temperature for 1 to 2 hours after the addition, cool down, discharge the reaction mixture from the bottom of the reaction tank, and centrifuge to obtain isoniazid p-aminosalicylate.

Embodiment 2

[0018] Put 15 kg of isoniazid in a reaction tank, add 300 kg of 20% (W / W) ethanol / water mixture as a solvent, heat to 55° C. and stir. After the isoniazid is completely dissolved, add 16.75 kg of p-aminosalicylic acid. Continue stirring at the same temperature for 1 to 2 hours after the addition, cool down, discharge the reaction mixture from the bottom of the reaction tank, and centrifuge to obtain isoniazid p-aminosalicylate.

Embodiment 3

[0020] Put 15 kg of isoniazid in a reaction tank, add 250 kg of 95% (W / W) ethanol / water mixture as a solvent, heat to 40° C. and stir. After the isoniazid is completely dissolved, add 16.75 kg of p-aminosalicylic acid. Continue stirring at the same temperature for 1 to 2 hours after the addition, cool down, discharge the reaction mixture from the bottom of the reaction tank, and centrifuge to obtain isoniazid p-aminosalicylate.

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Abstract

The present invention uses water or low-grade alcohol with a certain concentration as solvent, dissolves the isoniazid in the above-mentioned solvent, then adds the p-aminosalicylic acid, and adopts the processes of heating, stirring, cooling and separation so as to obtain the invented product pasiniazide.

Description

technical field [0001] The present invention relates to a compound preparation method, in particular to a drug synthesis method. Background technique [0002] The chemical structure of isoniazid p-aminosalicylate is shown below. [0003] [0004] Isoniazid has inhibitory and killing effects on Mycobacterium tuberculosis, but isoniazid can generate acetylated compounds in the body to be metabolically inactivated. The joint application of isoniazid and p-aminosalicylic acid can reduce the drug resistance of Mycobacterium tuberculosis and have a synergistic effect. Therefore, making isoniazid and p-aminosalicylic acid into isoniazid p-aminosalicylic acid can prevent and delay the acetylation of isoniazid, and play a synergistic anti-tuberculosis effect. Contents of the invention [0005] The object of the present invention is to provide a method for synthesizing isoniazid p-aminosalicylate. By adopting the method for synthesizing isoniazid p-aminosalicylate, the obtaine...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61P31/06C07D213/86
Inventor 张之君
Owner 张之君
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