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Valnemulin-O-benzoyl sulfonimide compound and preparation method thereof

A technology of benzoyl sulfonimide and benzoyl sulfonimide sodium, which is applied in the field of veterinary antibiotic preparation, can solve the problem of hygroscopic temperature and sensitivity to light, the dosage of the drug does not meet the requirements of the therapeutic dosage, and the impact on animal production. It can reduce the irritating odor of powder, improve bioavailability and improve animal palatability.

Inactive Publication Date: 2018-03-16
HUBEI LONGXIANG PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The current commercialized warnemulin mainly exists in the form of amorphous warnemulin hydrochloride. Because of its hygroscopicity, it is sensitive to temperature and light, and it is easy to decompose when it comes in contact with feed.
Moreover, the powder of warnemulin hydrochloride is highly irritating and has a strong smell. When it is used orally for the treatment of animal diseases, its palatability is relatively poor, which affects animal feed intake. , leading to the fact that wernimulin has not been popularized in the field of veterinary drug application so far

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Preparation of Vonimulin-o-benzoylsulfonimide complex

[0015] Put 7.23g of sodium o-benzoylsulfonimide into a 500mL three-necked flask, add 100mL of water and stir to dissolve, add 9% dilute hydrochloric acid dropwise to adjust the pH to 4-5, and add 150mL of ethyl acetate for extraction Layering, discarding the water layer, adding 11.3 g of Vonimulin to the organic layer, heating to 33 °C for 34 hours, cooling to 0-5 °C, stirring for half an hour, suction filtration, and vacuum drying at 46 °C for 11 hours, a total of 12.8 g of Vonimulin-o-benzoylsulfonimide complex were obtained.

Embodiment 2

[0017] Preparation of Vonimulin-o-benzoylsulfonimide complex

[0018] Put 9.64g of sodium o-benzoylsulfonimide into a 500mL three-necked flask, add 120mL of water and stir to dissolve, add 9% dilute hydrochloric acid dropwise to adjust the pH to 4-5, and add 150mL of dichloromethane for extraction Layering, discarding the water layer, adding 11.3 g of Vonimulin to the organic layer, warming up to 35°C for 30 hours, cooling to 0-5°C, stirring for half an hour, suction filtration, and vacuum drying at 50°C for 10 hours. 11.2 g of Vonimulin-o-benzoylsulfonimide complex were obtained.

Embodiment 3

[0020] Preparation of Vonimulin-o-benzoylsulfonimide complex

[0021] Put 12g of sodium o-benzoylsulfonimide into a 500mL three-necked flask, add 150mL of water to stir and dissolve, add 9% dilute hydrochloric acid dropwise to adjust the pH to 4-5, and add 200mL of tert-butyl methyl ether for extraction. layer, discard the water layer, add 11.3 g of Vonimulin to the organic layer, heat up to 37 °C for 26 hours, cool to 0 to 5 °C, stir for half an hour, suction filtration, and vacuum dry at 53 °C for 8 hours to obtain a total of 13.7 g of Vonimulin-o-benzoylsulfonimide complex.

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PUM

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Abstract

The invention provides a valnemulin-O-benzoyl sulfonimide compound. The compound is prepared by adopting a method comprising the following steps: firstly dissolving O-benzoyl sulfonamide in water, regulating a pH value to 4-5, adding an organic solvent for extraction, collecting an organic layer, then adding valnemulin into the organic layer for reaction, reducing the temperature to 0-5 DEG C after the end of reaction, performing suction filtration and collection on a solid precipitate and then drying to obtain the valnemulin-O-benzoyl sulfonimide compound. The valnemulin-O-benzoyl sulfonimidecompound provided by the invention solves the problem in the prior art, can improve the palatability of existing valnemulin hydrochloride, improve the bioavailability of the valnemulin and achieve the purpose of ensuring a clinical treatment effect.

Description

technical field [0001] The invention belongs to the technical field of veterinary antibiotic preparation, in particular to a vonimulin-o-benzoylsulfonimide compound and a preparation method thereof. Background technique [0002] Vonimulin is an animal-specific antibiotic officially launched in the 1990s. It belongs to the second-generation pleuromutilin semi-synthetic animal-specific antibiotic. It is mainly used for the prevention and treatment of hyodysenteriae and Mycoplasma pneumoniae caused by B. hyodysenteriae infection. Porcine endemic pneumonia caused by infection. Currently commercialized vornimulin mainly exists in the form of amorphous vornimulin hydrochloride. Because of its hygroscopicity and sensitivity to temperature and light, it is easy to decompose in contact with feeds. In addition, vonimulin hydrochloride powder is highly irritating and has a strong odor. When it is orally used for the treatment of animal diseases, its palatability is relatively poor, wh...

Claims

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Application Information

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IPC IPC(8): C07D275/06
CPCC07D275/06
Inventor 陈清平许灵艳郭熙昌王铭宏
Owner HUBEI LONGXIANG PHARMA TECH CO LTD
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