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Method for preparing tulathromycin compound

A technology of telamycin and compounds, which is applied in the field of preparation of telamycin compounds, can solve the problems of short half-life, gastrointestinal irritation, narrow antibacterial spectrum, etc.

Inactive Publication Date: 2013-05-01
QINGDAO VLAND BIOTECH INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the early macrolide antibiotics mainly have the following defects: irregular absorption, instability in gastric acid, short half-life, gastrointestinal irritation and narrow antibacterial spectrum, etc.
There are also many Gram-negative bacilli that are inherently resistant to macrolide antibiotics because they cannot effectively penetrate the outer membrane of the bacteria

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0018] The first step: substitution reaction:

[0019] Add 58.0 kg of demethylazithromycin (I) into a 500 L reaction tank, add 300 L of chloroform and 30.7 kg of pyridine, and cool to 0°C with refrigerated brine. Add 16.1 kg of acetic anhydride within 20 minutes, and keep the temperature of the reaction solution at about 0°C during the addition. After stirring for 2 hours, the temperature was raised to room temperature, and the reaction was stirred for another 12 hours. Add 100 L of saturated sodium bicarbonate aqueous solution and 2M NaOH aqueous solution to the reaction solution to adjust the pH of the reaction solution to 9.0, stir for 10 minutes and then stand to separate the layers, and remove the lower organic phase. The organic phase was washed once each with 50 L of water and 50 L of saturated brine, then dried by adding 1 kg of anhydrous magnesium sulfate, and filtered to remove magnesium sulfate. The filtrate was concentrated under reduced pressure at 45°C, placed ...

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PUM

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Abstract

The invention provides a method for preparing a tulathromycin compound. The method comprises the steps that: demethylated azithromycin is adopted as a raw material; and reactions such as substitution, oxidation, addition, reduction, condensation, and the like are carried out, such that a target compound is obtained. According to the invention, a cheaper raw material is adopted, and a traditional process employing low-temperature reaction is changed. The method has the advantages such as short process route, easy-to-control reaction, high yield, and the like. The method is suitable for large-scale industrialized productions.

Description

technical field [0001] The invention relates to a method for preparing a telamycin compound, which belongs to the field of veterinary medicine. Background technique [0002] Respiratory tract infection is one of the difficult-to-control infectious diseases in animal husbandry, which seriously harms animal husbandry production. When respiratory infection is prevalent, it will cause huge economic losses to livestock production. Therefore, how to prevent and treat respiratory infections in livestock such as pigs and cattle is an important research topic for veterinarians and veterinary medicine workers. Because respiratory tract infection is generally multi-infection, with many pathogenic factors and complex conditions, there is currently no very effective preventive method. For respiratory infections in animals, while seeking biological control and environmental blocking, drug control is still the main way at present. Seeking effective, safe, broad-spectrum, high-efficiency...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/00C07H1/00
Inventor 姚德勇郝智慧王艳玲
Owner QINGDAO VLAND BIOTECH INC
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