Catalyst, application and preparation method of trans-tranexamic acid

A technology of trans-tranexamic acid and tranexamic acid, which is used in the preparation of cyanide reactions, the preparation of organic compounds, organic chemical methods, etc., to reduce consumption, avoid the generation of barium sulfate solid by-products, and increase the proportion of Effect

Active Publication Date: 2022-03-25
JIANGSU TIANHE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] Purpose of the invention: In order to solve the problem of cis-trans conversion of tranexamic acid in the prior art, the present inventi...

Method used

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  • Catalyst, application and preparation method of trans-tranexamic acid
  • Catalyst, application and preparation method of trans-tranexamic acid

Examples

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preparation example Construction

[0024] 1. The preparation process of the hydrogenation reaction solution: add 1.5L of purified water, 50g of aminotoluic acid, and 24g of concentrated sulfuric acid into a 2L pressure reaction vessel, heat up to 50-60°C to dissolve the aminotoluic acid, then add 3.5g of platinum dioxide, Airtightly start to flow hydrogen, control the temperature at 50-60°C to react for 6 hours, cool down to room temperature and filter, the filtrate is the hydrogenation reaction liquid.

[0025] Two, the purity analysis of tranexamic acid adopts the following methods:

[0026] Chromatographic column: end-capped octadecylsilane bonded silica gel column C18 0.25m×4.6mm, 5μm

[0027] Flow rate: 0.9mL / min;

[0028] Detection wavelength: 210nm;

[0029] Injection volume: 40μL;

[0030] Column temperature: 30°C;

[0031] Run time: 2.5 times the retention time of tranexamic acid;

[0032] Mobile phase: Dissolve 11g of anhydrous sodium dihydrogen phosphate or 14.3g of dihydrogen sodium phosphate i...

Embodiment 1

[0035] Embodiment 1: Concentrate the aminotoluic acid hydrogenation reaction solution to about 20% of the mass concentration of tranexamic acid, add cesium hydroxide equivalent to 0.6 equivalents of aminotoluic acid added to the reaction system, heat up to 200 ° C, and keep the temperature Pressure reaction for 15 hours, the reaction is over, the reaction solution is concentrated to about 50% of the mass concentration of tranexamic acid, the ice water is cooled to about 10 ℃ to crystallize, and tranexamic acid is obtained by filtration. The purity of tranexamic acid is 99.2% by HPLC analysis. The body content is 0.4%.

Embodiment 2

[0036] Example 2: Concentrate the hydrogenation reaction solution of aminotoluic acid to about 30% of the mass concentration of tranexamic acid, add cesium oxide equivalent to 1 equivalent of aminotoluic acid added to the reaction system, raise the temperature to 150° C., keep the temperature and maintain the pressure After reacting for 20 hours, the reaction was completed. Concentrate the reaction solution until the concentration of tranexamic acid was about 50%, cooled the ice water to about 10°C to crystallize, and filtered to obtain tranexamic acid. The purity of tranexamic acid was 99.5% according to HPLC analysis. The content is 0.2%.

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Abstract

The invention discloses a catalyst, application and a preparation method of trans-tranexamic acid. The catalyst is cesium hydroxide or cesium oxide. The cesium hydroxide or cesium oxide is used for catalyzing the conversion of cis-tranexamic acid to trans-tranexamic acid, so that the conversion rate of cis-tranexamic acid to trans-tranexamic acid is increased, the refining difficulty of tranexamic acid is reduced, the product yield is increased, and the production cost is reduced.

Description

technical field [0001] The invention belongs to the technical field of production of crude drugs, and in particular relates to a catalyst, its application and a preparation method of trans-tranexamic acid. Background technique [0002] Tranexamic acid, also known as tranexamic acid, chemical name is p-aminomethylcyclohexanecarboxylic acid, molecular formula: C 8 h 5 NO 2 , belongs to the hemostatic drug, compared with the traditional hemostatic drug aminomethylbenzoic acid, tranexamic acid has a wider hemostatic range, rapid action, less side effects, and many clinical dosage forms, including small-volume injections, large-volume injections, tablets, and freeze-dried powder Injections, etc. are easy to use and have a wide range of uses. Not only are they widely used as first-line hemostatic drugs in various departments clinically, but they are also widely used as daily chemical products in daily life. They are added to skin care products and toothpaste. As the range of us...

Claims

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Application Information

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IPC IPC(8): B01J23/04C07C227/16C07C227/42C07C229/46
CPCC07C227/16C07C227/42B01J23/04C07C2601/14C07B2200/09C07C229/46
Inventor 刘磊周杰王仕林魏莉张嫚
Owner JIANGSU TIANHE PHARMA CO LTD
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