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Preparation method of tranexamic acid

A technology of tranexamic acid and aminomethylbenzoic acid, which is applied in the field of preparation of the hemostatic drug tranexamic acid, to reduce production costs and benefit the human body and the environment

Pending Publication Date: 2018-11-06
CHANGZHOU LANLING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0017] The purpose of the present invention is to solve the deficiencies of the existing p-aminomethylbenzoic acid method, to provide a method of tranexamic acid with lower production cost, more beneficial to the human body and the environment, higher yield, and suitable for industrialized large-scale production. Preparation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1）

[0032] The preparation method of the tranexamic acid of the present embodiment has the following steps:

[0033] ①Add 30.2g of p-aminomethylbenzoic acid (0.2mol), 180g of 5wt% sodium hydroxide aqueous solution (0.225mol) and 1.6g of ruthenium-carbon catalyst with 5wt% ruthenium content into the autoclave. Replace the air in the reaction kettle with nitrogen, then replace it with hydrogen, and then carry out catalytic hydrogenation at a temperature of 110°C and a pressure of 3.0 MPa. After the pressure no longer drops, keep the temperature for 2 hours, then cool down and filter to obtain p-Aminomethyl Cyclohexanecarboxylic acid cis-trans mixture (HPLC detection cis-trans ratio is about 85%:15%).

[0034] ②Add the cis-trans mixture of p-aminomethylcyclohexanecarboxylic acid obtained in step ① into the autoclave, replace the air in the reactor with nitrogen, and then carry out the conversion reaction at a temperature of 200°C and a pressure of 1.6MPa for 20h (The cis-trans ratio...

Embodiment 2～ Embodiment 4）

[0040] The preparation method of each embodiment is basically the same as that of Example 1, and the differences are shown in Table 1.

[0041] Table 1

[0042]

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PUM

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Abstract

The invention discloses a preparation method of tranexamic acid. According to the preparation method, the tranexamic acid is obtained through catalytic hydrogenation and conversion of p-aminomethylbenzoic acid, wherein the catalytic hydrogenation and the conversion are performed under an alkaline condition; the alkaline condition is constructed by adding sodium hydroxide or potassium hydroxide, ofwhich the molar amount is twice of that of the p-aminomethylbenzoic acid, only in the catalytic hydrogenation stage; the catalytic hydrogenation pressure is 2.5-3.0MPa; the catalytic hydrogenation temperature is 100-120 DEG C; a catalyst used during the catalytic hydrogenation is Raney nickel, a ruthenium carbon catalyst or a palladium carbon catalyst; the conversion pressure is 1.5-2.0MPa; the conversion temperature is 190-210 DEG C; after the conversion, p-toluenesulfonate formation and resin exchange refining are further included. The catalytic hydrogenation and the conversion under the alkaline condition are selected, so that the production cost can be reduced and benefits to a human body and the environment are higher; therefore, the preparation method is suitable for industrial massproduction.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to a preparation method of a hemostatic drug tranexamic acid. Background technique [0002] Tranexamic acid (also known as tranexamic acid, trans-4-aminomethylcyclohexanecarboxylic acid) is a good hemostatic drug, it is through the reversibility of lysine bound to the plasminogen molecule Blocking, resulting in an antifibrinolytic effect. Its hemostatic mechanism is the same as the hemostatic drug aminocaproic acid, and its hemostatic effect is 5-10 times stronger than that of aminocaproic acid. It is mainly used for upper gastrointestinal bleeding, bleeding, surgical bleeding and obstetrics and gynecology bleeding. In addition, tranexamic acid has a certain effect on the treatment of tonsil inflammation, tuberculosis and hemoptysis, acne, and chloasma. Although tranexamic acid is not a new drug, it is still the best irreplaceable hemostatic drug in the w...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C229/46C07C227/16
CPCC07C227/16C07C2601/14C07C229/46
Inventor 虞小平尹文娟徐永明
Owner CHANGZHOU LANLING PHARMA
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