Method for synthesizing aminomethylbenzoic acid

Abstract

The invention discloses a method for synthesizing aminomethylbenzoic acid. The method comprises the following step: with p-eormylbenzoic acid as an initial raw material, performing catalytic hydrogenation amination, thereby obtaining the aminomethylbenzoic acid, wherein the reaction temperature of catalytic hydrogenation amination is 80-150 DEG C; the reaction pressure of catalytic hydrogenation amination is 1.5-5.5MPa; ammonia water or an ammonia gas is adopted as an amination reagent of catalytic hydrogenation amination; a palladium-carbon catalyst is adopted as a catalyst of catalytic hydrogenation amination; the amount of the palladium-carbon catalyst accounts for 1-10% of the weight of the p-eormylbenzoic acid; and a step of refining treatment comprises alkali treatment, activated carbon decoloring and acid neutralization. The method disclosed by the invention is relatively short in synthesis route, relatively small in environment pollution, relatively low in production cost, freeof toxic material such as sodium cyanide or liquid chlorine, relatively high in security, relatively high in yield and applicable to industrial large-scale production.

Description

technical field [0001] The invention belongs to the technical field of medicine synthesis, and in particular relates to a synthesis method of a hemostatic drug, aminomethylbenzoic acid. Background technique [0002] Aminomethylbenzoic acid (also known as hemostatic arylic acid, p-aminomethylbenzoic acid) is a good hemostatic drug, which produces anti-lytic The role of fibrinogen. Its hemostatic mechanism is the same as the hemostatic drug aminocaproic acid, and its excretion is slow, its toxicity is low, and it is not easy to generate thrombus. It is mainly used for upper gastrointestinal bleeding, bleeding, surgical bleeding and obstetrics and gynecology bleeding. In addition, aminomethylbenzoic acid has a certain effect on the treatment of tonsil inflammation, tuberculosis and hemoptysis, acne, and chloasma. [0003] At present, the synthetic method of aminomethylbenzoic acid mainly contains following several kinds: [0004] 1. Taking p-nitrobenzoic acid as the startin...

AI Technical Summary

Problems solved by technology

[0005] The disadvantages of this method are: (1) the synthetic route is long and the total yield is low; (2) the reduction of iron powder + hydrochloric acid is more polluting to the environment; (3) the cyanidation reaction requires the use of highly toxic sodium cyanide, resulting in Low security; (4) Not suitable for large-scale industrial production

[0007] The disadvantages of this method are: (1) the synthetic route is also long, and the total yield is also low; (2) the chlorination reaction requires the use of highly toxic chlorine, resulting in low safety; (3) it is also not suitable for large-scale industrial production. Production

[0009] The disadvantages of this method are: (1) Both acid hydrolysis and ammoniation will produce more by-products, resulting in low yield; (2) Acid hydrolysis will produce a large amount of waste acid and waste water, which will seriously pollute the environment; (3) The post-ammoniation treatment is cumbersome, and it is also not suitable for large-scale industrial production