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Method for preparing tranexamicacid

A technology of tranexamic acid and aminotoluic acid is applied in the directions of organic chemical methods, cyanide reaction preparation, chemical instruments and methods, etc., can solve problems such as affecting efficiency, and achieve the effect of reducing reaction time and improving reaction efficiency

Active Publication Date: 2018-04-24
CHANGZHOU YINSHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since acid is used for catalytic hydrogenation and alkali is used for high-pressure conversion, acid adjustment is required after the hydrogenation reaction, which will affect the efficiency of synthesis

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] The method for preparing tranexamic acid in this embodiment includes the following steps:

[0018] Add 100kg of aminomethylbenzene, 1000kg of water, 90kg of concentrated sulfuric acid (with a concentration of 98%), and 3kg of platinum dioxide into the reaction kettle, keep the temperature at 60℃, and add excess hydrogen under stirring to carry out the hydrogenation reaction. After completion, water was concentrated to obtain a hydrogenation reaction liquid.

[0019] Add the tranexamic acid reaction solution after hydrogenation concentration to the reaction kettle, add 20kg of concentrated sulfuric acid, turn on the stirring, heat up to 185°C, control the pressure at 10Mpa, keep the temperature and stir for 2 hours, the reaction is over, add water to quench the reaction, After adjusting the pH value to 7.0, a large amount of solids precipitated, and after filtration, a tranexamic acid product was obtained. HPLC content> 96%, the yield is 89%.

[0020] The reaction formula is ...

Embodiment 2

[0023] The method for preparing tranexamic acid in this embodiment includes the following steps:

[0024] Add 100kg of aminomethylbenzoic acid, 1500kg of water, 100kg of concentrated sulfuric acid (98% concentration), and 2.5kg of platinum dioxide into the reactor, keep the temperature at 55°C, and pass in excess hydrogen under stirring to carry out the hydrogenation reaction. After the reaction, the water was concentrated to obtain a hydrogenation reaction liquid.

[0025] Add the tranexamic acid reaction solution after hydrogenation concentration into the reaction kettle, add 10kg of concentrated sulfuric acid, turn on the stirring, heat up to 190°C, control the pressure at 11Mpa, keep and stir for 1.5 hours, the reaction is over, add water to quench the reaction, After adjusting the pH value to 7.0, a large amount of solids precipitated, and after filtration, a tranexamic acid product was obtained. HPLC content> 96%, 87% yield.

Embodiment 3

[0027] The method for preparing tranexamic acid in this embodiment includes the following steps:

[0028] Add 100kg of aminomethylbenzoic acid, 1500kg of water, 100kg of concentrated sulfuric acid (98% concentration), and 2.5kg of platinum dioxide into the reactor, keep the temperature at 55°C, and pass in excess hydrogen under stirring to carry out the hydrogenation reaction. After the reaction, the water was concentrated to obtain a hydrogenation reaction liquid.

[0029] Add the tranexamic acid reaction solution after hydrogenation concentration into the reaction kettle, add 10kg of concentrated sulfuric acid, turn on the stirring, heat up to 195°C, control the pressure at 12Mpa, keep the temperature and stir for 1 hour, the reaction is over, add water to quench the reaction, After adjusting the pH value to 7.0, a large amount of solids precipitated, and after filtration, a tranexamic acid product was obtained. HPLC content> 96%, 88% yield.

[0030] The reagents used in the pres...

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PUM

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Abstract

The invention relates to a method for preparing tranexamicacid. The method comprises the following steps: adding the aminomethylbenzoic acid, water, concentrated sulfuric acid and a catalyst into a reaction vessel for stirring and heating; then introducing hydrogen for carrying out hydrogenation reaction to obtain hydrogenated reaction liquid; adding the hydrogenated reaction liquid and the concentrated sulfuric acid into the reaction vessel, raising the temperature to 180 to 200 DEG C, and carrying out heat-preservation stirring and conversion reaction to obtain the tranexamicacid. The methodfor preparing the tranexamicacid, disclosed by the invention, has the advantages of simplified technology, short reaction time and high synthesis efficiency.

Description

Technical field [0001] The invention relates to a process method for preparing tranexamic acid and belongs to the technical field of chemical synthesis. Background technique [0002] Tranexamic acid is an anti-fibrinolytic amino acid, which can compete against plasmin activator, so that plasminogen cannot be converted into plasmin, and has the proteolytic activity of inhibiting plasmin. The effect is similar to that of amino toluic acid. It has a good effect on bleeding caused by increased fibrinolytic activity, and the effect is about twice that of amino toluic acid. [0003] The existing commonly used tranexamic acid synthesis process is to first carry out catalytic hydrogenation of carboxybenzylamine, and then carry out high-pressure conversion with alkali. Since catalytic hydrogenation uses acid and high-pressure conversion uses alkali, acid adjustment is required after the completion of the hydrogenation reaction, which will affect the efficiency of synthesis. Summary of the...

Claims

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Application Information

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IPC IPC(8): C07C229/46C07C227/16C07C227/32
CPCC07B2200/07C07C227/16C07C227/32C07C229/46
Inventor 陶鑫韩加齐潘利俊葛柏凯焦丹丹
Owner CHANGZHOU YINSHENG PHARMA
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