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Tranexamic acid preparation method

A technology of tranexamic acid and aminotoluic acid, which is applied in the preparation of organic compounds, organic chemical methods, cyanide reaction preparation, etc., can solve the problems of reducing the service life of platinum catalysts, increasing production costs, and reducing production efficiency. The effect of shortening the indexing time, reducing the pressure on environmental protection and improving the service life

Active Publication Date: 2018-10-23
周道平
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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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Embodiment 1

[0033] A preparation method of tranexamic acid in the embodiment of the present invention, comprising:

[0034] (1) Mix 50 kg of aminotoluic acid with 300 L of pure water, slowly add 10 L of concentrated sulfuric acid under stirring conditions, heat to 100 ° C, dissolve the aminotoluic acid, cool and crystallize, and filter to obtain the pretreated aminotoluic acid;

[0035] (2) add sulfuric acid solution and metallic platinum catalyst, adjust pH to 1~3, carry out hydrogenation reaction to the pretreated aminotoluic acid, remove redundant sulfuric acid, obtain hydrogenation product;

[0036] (3) Add barium hydroxide and pure water to the hydrogenation product, control the mass ratio of the hydrogenation product to barium hydroxide to 1:3, raise the temperature to 200°C, and perform high-temperature transposition reaction on the hydrogenation product. The reaction time is 10h, to obtain tranexamic acid.

[0037] Table 1 is the high performance liquid chromatography (HPLC) resu...

Embodiment 2

[0045] A preparation method of tranexamic acid in the embodiment of the present invention, comprising:

[0046] (1) Mix 50 kg of aminotoluic acid with 300 L of pure water, slowly add 10 L of concentrated sulfuric acid under stirring conditions, heat to 105° C., dissolve the aminotoluic acid, cool and crystallize, and filter to obtain the pretreated aminotoluic acid;

[0047] (2) add sulfuric acid solution and metallic platinum catalyst, adjust pH to 1~3, carry out hydrogenation reaction to the pretreated aminotoluic acid, remove redundant sulfuric acid, obtain hydrogenation product;

[0048] (3) Add barium hydroxide and pure water to the hydrogenation product, control the mass ratio of the hydrogenation product to barium hydroxide to 1:4, raise the temperature to 190°C, and perform high-temperature transposition reaction on the hydrogenation product. The reaction time is 10h, to obtain tranexamic acid.

[0049] Aminotoluic acid raw material is through pretreatment, and the hi...

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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...

Claims

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Application Information

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IPC IPC(8): C07C229/46C07C227/16C07C227/30
CPCC07B2200/07C07C227/16C07C227/30C07C2601/14C07C229/46
Inventor 周道平
Owner 周道平
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