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Preparation method of isoniazid para-aminosalicylate

A technology of isoniazid p-aminosalicylic acid and sodium aminosalicylate, applied in the field of preparation of isoniazid p-aminosalicylic acid, can solve the problem that the properties of aminosalicylic acid are unstable, it is difficult to buy pure finished products, Affect the production process and other problems to achieve the effects of stable quality and yield, good water solubility, and reduced raw material consumption

Active Publication Date: 2012-02-08
CHONGQING HUABANGSHENGKAI PHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, p-aminosalicylic acid, one of the raw materials used in this patent, is inconvenient to store due to its unstable properties.
And usually contain more impurities, it is difficult to buy finished products with higher purity
If p-aminosalicylic acid containing more impurities is directly used as a raw material, it will not only affect the quality of the product, but also affect the production process; in addition, the yield of the product in this patented method is only 70%, so it is not convenient for industrial production

Method used

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  • Preparation method of isoniazid para-aminosalicylate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Add 100kg of sodium p-aminosalicylate into 250kg of purified water, stir, add hydrochloric acid, adjust the pH to 3.5, add 700kg of ethyl acetate, after sufficient extraction, separate layers, discard the water layer and wash the extract with water. Add 65 kg of isoniazid to the extract, stir and raise the temperature to 75-80°C, react for 40 minutes, cool down to -10-5°C, keep warm and crystallize for 80 minutes. After centrifugation, the obtained solids are boiled and dried at 60-65°C to obtain the finished product of isoniazid p-aminosalicylic acid, which is a bright yellow rhombic crystal. The finished product content is 98.5%, and the yield is 97%.

Embodiment 2

[0032] Add 100kg of sodium p-aminosalicylate into 150kg of purified water, stir, add sulfuric acid, adjust the pH to 4.0, add 850kg of propyl acetate, after fully extracting, separate layers, discard the water layer and wash the extract with water. Add 60kg of isoniazid to the extract, stir and heat up to 65-70°C, react for 40 minutes, cool down to 5-10°C, and keep warm for 120 minutes for crystallization. After centrifugation, the obtained solid is boiled and dried at 65-70°C to obtain the finished product of isoniazid p-aminosalicylic acid, which is a bright yellow diamond-shaped crystal. The finished product content is 98.3%, and the yield is 95%.

Embodiment 3

[0034] Add 100kg of sodium p-aminosalicylate into 200kg of purified water, stir, add hydrochloric acid, adjust the pH to 3.5, add 700kg of methyl formate, after sufficient extraction, separate layers, discard the water layer and wash the extract with water. Add 50kg of isoniazid to the extract, stir and heat up to 50-55°C, react for 30 minutes, then cool down to -5-0°C, keep warm and crystallize for 80 minutes. After centrifugation, the resulting solid is boiled and dried at 50-55°C to obtain the finished product of isoniazid p-aminosalicylic acid, which is a bright yellow diamond-shaped crystal. The finished product content is 98.1%, and the yield is 92%.

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Abstract

The invention discloses a preparation method of isoniazid para-aminosalicylate. The preparation method comprises that a sodium para-aminosalicylate solution is added with an acid and then is extracted by an organic solvent and isoniazid is added into the extract to produce a desired product. The isoniazid para-aminosalicylate product prepared by the preparation method has isoniazid para-aminosalicylate purity above 98%. Through the preparation method, a yield of 90 to 98% is obtained. The preparation method adopts simple and environmentally friendly processes, realizes recycle of an extraction solvent and saves greatly costs.

Description

Technical field: [0001] The invention relates to a preparation method of isoniazid p-aminosalicylate. Background technique: [0002] Isoniazid p-aminosalicylic acid is an anti-tuberculosis drug chemically synthesized from p-aminosalicylic acid and isoniazid by a unique method (as shown in formula 1). A mixture of niacin. Its anti-tuberculosis effect belongs to the isoniazid type, and its clinical effect is equivalent to or better than that of isoniazid with increased doses of p-aminosalicylic acid, or with the same effect of mixed treatment with isoniazid and streptomycin. The drug has low toxicity, good tolerance, and rarely causes adverse reactions such as gastrointestinal discomfort or neuritis. [0003] [0004] Formula 1 [0005] Patent ZL03135204.9 uses p-aminosalicylic acid and isoniazid as raw materials, uses water or a certain concentration of lower alcohol as a solvent, and obtains p-aminosalicylic acid isoniazid after heating, stirring, cooling and separatio...

Claims

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Application Information

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IPC IPC(8): C07D213/86C07C229/64C07C227/14
Inventor 李国杨
Owner CHONGQING HUABANGSHENGKAI PHARM
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