Method of manufacturing 1-(2-methoxyphenyl)-3-naphthyl group-2-urea

A technology of naphthyl and naphthylamine, applied in the direction of amide active ingredients, organic chemistry, antibacterial drugs, etc., can solve the problems of enhanced drug resistance of pathogenic bacteria, reduce drug costs, reduce minimum inhibitory concentration, and solve resistance The effect of the drug on bacterial infection

Active Publication Date: 2008-01-23
PU LIKE BIO ENG
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Problems solved by technology

[0003] In order to solve the problem that the drug resistance of existing pathogenic bacteria is increasing day by day, the purpose of the present invention is to provide a preparation method of bacterial resistance inhibitor INF271, so that the antibacterial and synergistic effect of the new bacterial resistance inhibitor is better, so that animals Major bacterial infections and diseases can be better and effectively controlled, reducing drug costs and improving the safety of animal-derived foods

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  • Method of manufacturing 1-(2-methoxyphenyl)-3-naphthyl group-2-urea
  • Method of manufacturing 1-(2-methoxyphenyl)-3-naphthyl group-2-urea
  • Method of manufacturing 1-(2-methoxyphenyl)-3-naphthyl group-2-urea

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specific Embodiment approach 2

[0018] The reaction process is: (1) 143.2g of β-naphthylamine and 62g of urea were added to 300ml of dilute sulfuric acid, heated to reflux for 2 hours, cooled and filtered to obtain 179g of 1-(naphthalene-2 ​​base)-urea. Yield 96%.

[0019] Reaction (2) 186.2g of 1-(naphthalene-2 ​​base)-urea was mixed with 125g of anisole and 300ml of dilute sulfuric acid, heated to 100°C for 3 hours, cooled, and filtered to obtain 1-(2-methoxy 270 g of phenyl)-3-naphthyl-2-urea. The total yield of the two-step reaction is 88%.

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Abstract

A preparation method of the bacterial drug-resistant inhibitor is provided, which is that the Beta-naphthamine is utilized as raw material and reacts with the urea to gain the N-(2-naphthol)- thiourea, and then reacts with the o-amino pheylmethyl ether to gain INF271, namely, 1-(2- methoxyphenyl)-3-naphthyl-2-thiourea. (1) The Beta-naphthamine and urea are added in water and are added with the diluted acid for 1h to 5h heating and reflux and are filtered after cooling to gain 1-(naphthol-2base)-thiourea; (2) 1-(naphthol-2base)-thiourea and the o-amino pheylmethyl ether mix with the diluted acid and are heated to 100 DEG C. to 108 DEG C., and then react for 1h to 5h to gain the 1-(2- methoxyphenyl)-3-naphthyl-2-thiourea after cooling and filtering. The diluted acid applied in the reaction can be sulphuric acid, hydrochloric acid and acetic acid, etc. the priority is hydrochloric acid.

Description

Technical field: [0001] The invention belongs to the preparation technology of veterinary medicine, in particular to a preparation method of 1-(2-methoxyphenyl)-3-naphthyl-2-urea. Background technique: [0002] Due to the continuous and extensive application or even abuse of antibacterial drugs in animal breeding practice, coupled with the objective existence of cross-resistance of antibacterial drugs shared by humans and animals, the drug resistance of pathogenic bacteria is increasing day by day, and the efficacy of many drugs is rapidly declining. Under stress, bacteria develop resistance to almost all clinically used antimicrobials. According to the results of the general survey of bacterial drug resistance by relevant institutions, the drug resistance of Staphylococcus aureus to erythromycin, chloramphenicol, and tetracycline is as high as 80%, 70%, and 60%, respectively, and Escherichia coli is resistant to gentamicin, sulfa , erythromycin resistance as high as 70%, 6...

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C275/34A61K31/17A61P31/04
Inventor 刘兴金翟孝忠张永奎宫亮张晓会赵彦语
Owner PU LIKE BIO ENG
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