Method of producing toltrazuril

A technology of toltrazuril and reaction, applied in the direction of organic chemistry, etc., can solve problems such as increased drug resistance of coccidia

Active Publication Date: 2008-01-23
PU LIKE BIO ENG +1
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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
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  • Method of producing toltrazuril

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preparation example Construction

[0040] The preparation process of toltrazuril:

[0041] Reaction 1: Mix 410g of methanol and 158g of p-nitrochlorobenzene to fully melt, and add dropwise a mixture of sulfur, sodium sulfide and methanol. Keep at 60-65°C for 2 hours, cool down, add 880g 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, 153.6 g of methyl sulfide was obtained by spin filtration. The yield was 91.1%.

[0042] Reaction 2: 1800g of chloroform and 400g of methyl sulfide, stir evenly, control the temperature at 75-80°C, let the chlorine gas react for about 3 hours, and filter to obtain 600.9g of chlorinated compounds. The yield was 92.7%.

[0043] Reaction 3: Add 52g of antimony trifluoride to 200g of chlorinated substance and react at 40-60℃ to obtain fluoride; 1226g of water, 277g of iron powder, 24g of hydrochloric acid, and 14g of ammonium chloride. -50°C, add fluoride, stir and heat to reflux for 2 hours,...

specific Embodiment approach 2

[0051] Reaction 1: Mix 500 g of methanol and 158 g of p-nitrochlorobenzene until it is fully dissolved, and add dropwise a mixture of sulfur, sodium sulfide and methanol. Keep at 60-65°C for 2 hours, cool down, 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 spin filtration. The yield was 91.6%.

[0052] Reaction 2: 2000g chloroform and 400g methyl sulfide, stir evenly, control the temperature between 70-75°C, let the chlorine gas react for about 3.5 hours, and filter to obtain 598.3g chloro compound. The yield was 92.3%.

[0053] Reaction 3: Add 52g of antimony trifluoride to 200g of chlorinated substance and react at 40-60℃ to obtain fluoride; 1226g of water, 277g of iron powder, 24g of hydrochloric acid, and 14g of ammonium chloride. -50°C, add fluoride, stir and heat to reflux for 2 hours, perform steam distillation, and steam u...

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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 technical field of preparation of veterinary drugs, and mainly proposes a preparation method of toltrazuril. Background technique: [0002] Coccidiosis is the most common and most aggressive disease in livestock and poultry. The harm to the breeding industry is quite serious. In addition, the occurrence of this disease often causes the body's resistance to decline, and it is often accompanied or secondary to infections. Bacterial 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 drugs for prevention and treatment of coccidiosis are: all drugs on the market are rarely used. Within a few days, as long as 1-3 years, the coccidia quickly develop drug resistance. Most drugs not only have toxic side effects on livestock and poultry, but also remain in meat and eggs and other produ...

Claims

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Application Information

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Patent Type & Authority Applications(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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