Producing method of of tranexamic acid

Abstract

The invention discloses a process for producing tranexamic acid, wherein p-aminomethyl benzoic acid raw material is hydrogenised, and the hydrogenization liquid is neutralized to pH7-7.5 through barium carbonate, after filtering, the solution is condensed to 10 gram molecule p-aminomethyl benzoic acid reaction liquid of 5l, then charge raw materials by the portion ratio of ammonia cyclohexyl-methane carboxyl acid sym-form liquid (V) : barium hydroxide (W) : water (W) : ethanol (V) = 1:0.5-1.5:2-3.5:1.5-3, elevating the temperature to 230-260 deg. C, the pressure being 2.9-4.8.0Mpa, reacting time being 7.5-10 hours, after reaction charging water and elevating the temperature to 60-70 deg. C, neutralizing through carbon dioxide till pH=6-7.5, filtering and adjusting pH=5.2-5.5 through sulfuric acid, stewing, charging right amount activated charcoal, boiling and decolorizing, filtering, filter cake washing, condensing, charging ethanol for recrystallization, cooling down to 8-12 deg. C, filtering, washing crystallization by ethanol, filter cake drying to obtain tranexamic acid.

Description

technical field [0001] The invention relates to a production method of tranexamic acid (also known as tranexamic acid). Background technique [0002] For many years, the production methods of tranexamic acid in China have two methods: method A, namely the methyl acrylate method and method B, namely the p-carboxybenzylamine method. In 1980, the "National Compendium of Raw Materials and Processes" edited by the State Administration of Medicine published P510-512 The operating standards are given on the page. [0003] Method A was originally used by Shanghai, Jiangsu and other manufacturers. Because this method uses highly toxic cyanide banned by the state as raw material, it has basically stopped using it at present. [0004] The production steps and process conditions of method B are as follows: [0005] ①, catalytic hydrogenation [0006] Ingredients ratio p-carboxybenzylamine (W): platinum dioxide (W): sulfuric acid (V): water (V) = 1: 0.05: 0.56: 33 ...

AI Technical Summary

Problems solved by technology

In a word, so far, the production methods of tranexamic acid both at home and abroad have a cis-isomer content of more than 0.5% no matter the method A or method B, and its quality has not reached the Chinese Pharmacopoeia 2000 edition, the British Pharmacopoeia 93 edition, and the Japanese Pharmacopoeia Bureau. The 13th edition and the European Pharmacopoeia 2000 edition require that the cis-body content not exceed 0.5%

And its conversion reaction time of the production method of prior art tranexamic acid is long, and the unit productive rate is that labor productivity is not high, simultaneously, because the waste barium sulfate that needs discarding is generated twice in the production process, and raw material consumption is increased