A kind of preparation method of tranexamic acid

Abstract

The invention discloses a tranexamic acid preparation method, and belongs to the technical field of drug synthesis. The preparation method includes the steps: (1) mixing aminomethylbenzoic acid and pure water, slowly adding concentrated sulfuric acid under the condition of stirring, heating mixture to preset temperature and performing cooling crystallization and filtration to obtain pretreated aminomethylbenzoic acid; (2) adding sulfuric acid solution and catalysts, performing hydrogenation reaction on the pretreated aminomethylbenzoic acid and removing residual sulfuric acid to obtain a hydrogenated product; (3) adding alkali and the pure water into the hydrogenated product, controlling the weight ratio of the hydrogenated product to the alkali to be 1:(3-6), heating the mixture to set temperature, and performing transposition reaction on the hydrogenated product to obtain tranexamic acid. According to the tranexamic acid preparation method, the aminomethylbenzoic acid is pretreated to decrease the content of organic amine and ferrum in raw materials, the service life of the catalysts is prolonged, and production cost is greatly reduced. The adding proportion of the alkali is properly increased, so that the proportion of trans-tranexamic acid in a transposition product, and transposition time is shortened.

Description

technical field [0001] The invention belongs to the technical field of drug synthesis, and in particular relates to a preparation method of tranexamic acid. Background technique [0002] The chemical name of tranexamic acid is: trans-4-aminomethylcyclohexanecarboxylic acid (Tranexamic Acid), the molecular formula is C 8 h 15 NO 2 , the molecular weight is 157.21, and the structural formula is as follows: [0003] [0004] Tranexamic acid is white crystalline powder, odorless, slightly bitter taste, easily soluble in water, almost insoluble in ethanol and acetone, tranexamic acid can bind to the fibrin affinity site on plasmin and plasminogen The lysine binding site (LBS) of plasmin is strongly adsorbed, which inhibits the binding of plasmin, plasminogen and fibrin, thereby strongly inhibiting the decomposition of fibrinolysis caused by plasmin; in addition, macroglobules in serum In the presence of protein and other anti-fibrinolytic enzymes, the anti-fibrinolytic eff...

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Problems solved by technology

[0005] At present, the process for preparing tranexamic acid in industry is: first carry out catalytic hydrogenation of aminotoluic acid, then carry out high-pressure conversion under alkaline conditions, and carry out hydrogenation reaction through platinum catalysts. Due to the residual organic amine in aminotoluic acid 1. Trace amounts of iron will poison the catalyst, greatly reducing the service life of the platinum catalyst, thus increasing the production cost; during the alkaline high-pressure conversion, the conversion cycle is longer due to the low addition of alkali, which reduces the production efficiency and the product low yield

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