Preparation method of isoniazid para-aminosalicylate

Abstract

The invention relates to a preparation method of isoniazid para-aminosalicylate. The preparation method of isoniazid para-aminosalicylate comprises the following steps: (1) respectively weighting water and an organic solvent, mixing, adding para-aminosalicylic acid and isoniazid to a solvent of the water and the organic solvent, heating and stirring; (2) cooling and growing grains, and filtering to obtain isoniazid para-aminosalicylate, wherein the organic solvent is an organic ester with the carbon number of less than or equal to 6. By using the preparation method, the preparation of isoniazid para-aminosalicylate is realized at low cost and high efficiency in a water and ester two-phase solvent system under a simple, convenient and feasible technological condition. The content of isoniazid para-aminosalicylate prepared by the method is higher than 99%. Isoniazid para-aminosalicylate has good appearance crystal form, standard color and luster and good stability. The preparation method has the advantages of few reaction operating units, simple technological process, short time consumption, low production cost, environmental friendliness, simple operation and easiness for control on the implementation process and is suitable for the industrial production of isoniazid para-aminosalicylate.

Description

【Technical field】 [0001] The invention relates to the technical field of chemical pharmacy, in particular, the invention relates to a preparation method of isoniazid p-aminosalicylate. 【Background technique】 [0002] The chemical name of isoniazid p-aminosalicylate is 4-pyridinecarbohydrazide-4-aminosalicylic acid, the common name is pasniazid, the alias is hydrazine, and the chemical formula is C 13 h 14 0 4 N 4 , the structural formula is: [0003] [0004] Isoniazid p-aminosalicylate is a chemical compound of isoniazid and p-aminosalicylic acid, yellow crystalline powder. The p-aminosalicylic acid in this product can effectively delay and block the acetylation process of isoniazid in the body, and maintain a higher and longer isoniazid concentration in the blood, and its curative effect is equivalent to or better than that of isoniazid. Increased dose of niazid has the same curative effect on aminosalicylic acid or streptomycin plus isoniazid mixed treatment, and ...

AI Technical Summary

Problems solved by technology

In the above two patents, the water and (or) alcohol reaction solvent used in the Chinese patent ZL03135204.9, the raw material p-aminosalicylic acid is difficult to dissolve in it, so that there is unreacted p-aminosalicylic acid in the finished product, resulting in The product is unstable and easy to degrade and deteriorate, resulting in unqualified indicators such as its color, content and melting point; Chinese patent application ZL201010241108.1 uses sodium p-aminosalicylate as a raw material, and it is necessary to acidify the aqueous solution of sodium p-aminosalicylate and use a hydrophobic organic solvent extraction, then adding isoniazid to generate isoniazid p-aminosalicylate, and there are many production steps; both of them use a single system (hydrophilic or hydrophobic) as the solvent for preparing isoniazid p-aminosalicylate. Unreacted raw materials are mixed into the finished product, resulting in the instability of the finished product, easy degradation and deterioration, resulting in unqualified indicators such as color, content and melting point

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