Preparation method for 1-methyl-5-[3-methyl-4-(4-trifluoromethylthio-phenoxy)-phenyl]-biuret, and application thereof

A technology of trifluoromethylthio and phenoxy, applied in 1-methyl-5-[3-methyl-4-(4-trifluoromethylthio-phenoxy)-phenyl]-condensate The preparation and application of diurea can solve the problems of poor safety and low yield, and achieve the effects of mild conditions, high conversion rate and simple process
CN102731351AActive Publication Date: 2012-10-17ZHEJIANG GUOBANG PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ZHEJIANG GUOBANG PHARMA
Publication Date
2012-10-17

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Abstract

The present invention mainly discloses a preparation method for 1-methyl-5-[3-methyl-4-(4-trifluoromethylthio-phenoxy)-phenyl]-biuret, and an application thereof. According to the present invention, 3-methyl-4-(4-trifluoromethylthio-phenoxy)-aniline reacts with a cyanate in the presence of an acid to obtain N-[3-methyl-4-(4-trifluoromethylthio-phenoxy)-phenyl]-urea; the N-[3-methyl-4-(4-trifluoromethylthio-phenoxy)-phenyl]-urea reacts with methylaminoformyl chloride in a solvent to obtain 1-methyl-5-[3-methyl-4-(4-trifluoromethylthio-phenoxy)-phenyl]-biuret; the 1-methyl-5-[3-methyl-4-(4-trifluoromethylthio-phenoxy)-phenyl]-biuret and diethyl carbonate are subjected to condensation under an alkaline condition to obtain an anti-coccidian drug toltrazuril. The method of the present invention has characteristics of simple process, mild conditions, high total conversion rate, good product quality, cheap and available raw materials, and green environmental protection, and is a competitive industrialization synthesis route.
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Description

technical field

[0001] The present invention relates to a key intermediate of toltrazuril, 1-methyl-5-[3-methyl-4-(4-trifluoromethylthio-phenoxy)-phenyl]-biuret Preparation. Background technique

[0002] Toltrazuril is an anticoccidial drug developed by Bayer AG in Germany in the late 1980s, with a trade name of Baycox (Baiqiuqing). It interferes with the division of the parasite nucleus and mitochondrial respiratory metabolism, killing coccidia in all stages of intracellular development. It has a broad spectrum of insect resistance, and has a high curative effect on coccidia in chickens, geese and pigeons, and is highly effective against mild and severe coccidia infections.

[0003] The synthetic method of toltrazuril has many bibliographical reports, and wherein comparatively having industrial value is to use 1-methyl-5-[3-methyl-4-(4-trifluoromethylthio-phenoxy)- Phenyl]-biuret (abbreviated as biuret hereinafter) is an intermediate, which carries out ring closure react...

Claims

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