Method of producing toltrazuril

A toltrazuril and reaction technology, applied in organic chemistry and other fields, can solve problems such as enhanced drug resistance of coccidia

Active Publication Date: 2011-06-29
PU LIKE BIO ENG +1
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  • Claims
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Problems solved by technology

[0003] In order to solve the problem that the drug resistance of existing coccidia is increasing day by day, the present invention provides a preparation method of toltrazuril, so that toltrazuril can realize industrialized production smoothly, thereby effectively controlling the occurrence and development of cecal coccidia. Death, even can kill all coccidia oocysts

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  • Method of producing toltrazuril
  • Method of producing toltrazuril
  • Method of producing toltrazuril

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specific Embodiment approach 2

[0049] Reaction 1: Mix 500g of methanol and 158g of p-nitrochlorobenzene and heat up to complete dissolution, then add sulfur, sodium sulfide, and methanol mixture dropwise. Keep at 60-65°C for 2 hours, lower the temperature, add 1000g of water, let cool, add 192g of dimethyl sulfate dropwise, and adjust the pH to greater than 9 with sodium hydroxide solution. After the reaction, 154.5 g of methyl sulfide was obtained by shaking filtration. Yield 91.6%.

[0050] Reaction 2: 2000g chloroform, 400g methyl sulfide, stir evenly, control the temperature between 70-75°C, react with chlorine gas for about 3.5 hours, and filter to obtain 598.3g of chlorinated compound. Yield 92.3%.

[0051] Reaction 3: Add 52 g of antimony trifluoride to 200 g of chlorinated compounds and react at a temperature of 40-60 ° C to obtain fluorinated compounds; 1226 g of water, 277 g of iron powder, 24 g of hydrochloric acid, and 14 g of ammonium chloride; -50°C, add fluoride, stir and heat up to reflux...

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Abstract

A preparation method of the Toltrazuril is provided. The Toltrazuril is the 1-[3-methyl-4-(4- Trifluoromethylthiobenzoxy) benzyl]-3-methyl-1, 3, 5, -triazine-2, 4, 6(1H, 3H, 5H)-trione. The methyl sulfide chloro compounds, fluoro-compounds, amides, phenol, methyl nitrate chlorobenzene, benzene aether, ammonia benzene aether, isonitrile acid ester and methyl urea from the reactions of 4-nitrochlorobenzene, sulfur, sodium sulfide and dimethyl sulfate. The detailed preparation is that reaction 1: the methanol of 410g and 4-nitrochlorobenzene of 158g are mixed and heated until soluble and are added with sulfur, sodium sulfide and methanol mixed liquor by drops, and kept for 2h under temperature of 60 DEG C. to 65DEG C.; reduce the temperature, add water of 880g and add dimethyl sulfate of 192g; during the period, the pH value of the sodium hydroxide is adjusted over 9, and the methyl sulfide of 153.6 is gained by filtering after reaction with yield of 91.1 per cent.

Description

Technical field: [0001] The invention belongs to the veterinary drug preparation technology, and mainly proposes an improved method for preparing toltrazuril. Background technique: [0002] Coccidiosis is the most common and most invasive disease in livestock and poultry, and it is very harmful to the breeding industry. In addition, the occurrence of this disease often causes the body's resistance to decline, and it is often associated with or secondary infection of various diseases. Bacteroid-like diseases have brought great difficulties to clinical diagnosis and treatment. At present, the main means to control this disease is still to take drug prevention and treatment. The main problems of current drug prevention and treatment of coccidiosis are: all marketed drugs are less effective after administration. In a few days, as many as 1-3 years, the coccidia quickly develop drug resistance. Most drugs not only have toxic and side effects on livestock and poultry, but also rem...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D251/30
Inventor 张许科刘兴金杨会鲜吕锁群朱华伟张晓会赵秋君栗子丰
Owner PU LIKE BIO ENG
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