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A kind of method for preparing high-purity fidaxomicin

A fidaxomicin, high-purity technology, applied in the preparation of sugar derivatives, chemical instruments and methods, organic chemistry, etc., can solve the problems of large initial investment, high operating costs, and cumbersome operations, and achieve low operating costs and reduced The effect of simple production cost and operation method

Active Publication Date: 2018-09-28
CHONGQING QIANTAI BIOLOGICAL MEDICINE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method requires two silica gel column chromatography and ODS reversed-phase medium pressure liquid chromatography, which is cumbersome and expensive
[0010] The equipment of preparative chromatography is used in the prior art, but this equipment has the disadvantages of large initial investment and high operating cost

Method used

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  • A kind of method for preparing high-purity fidaxomicin
  • A kind of method for preparing high-purity fidaxomicin
  • A kind of method for preparing high-purity fidaxomicin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] 80L fermented broth (HPLC chromatogram as figure 1Shown) pressure filtration obtains 28.5kg mycelia. Add 90L of 70% ethanol solution to the mycelium, stir for 5 hours, and filter to obtain 94.3L of filtrate, which contains 187g of fidaxomicin through HPLC detection. Dilute the filtrate with purified water to an ethanol concentration of 50%, then introduce it into SP825L adsorption resin with a capacity of 20L, pre-wash the resin with 40L of 60% ethanol solution at a flow rate (1BV / h), and then wash it with 100L of 70% ethanol solution Desorption, flow rate (1BV / h), collect one component per 2L, and mix the components with a purity above 70%. The mixed components were then concentrated under reduced pressure to an ethanol concentration of 13%. Stand still and cool to 15°C, filter with suction, and dry to obtain 224g yellow solid, yield 71.8%, HPLC: 76.7% (HPLC such as figure 2 shown).

Embodiment 2

[0041] Dissolve 224g of the yellow solid obtained in Example 1 in 3.5L of ethyl acetate, dissolve, cool down to 5°C, drop 2.3L of 5°C petroleum ether into the above-mentioned ethyl acetate solution under stirring, and keep The temperature was stirred at 3-8°C for 5 hours. Filter, filter cake is vacuum-dried, obtain off-white powder 192g, yield 85%, HPLC: 77.3% (HPLC chromatogram such as image 3 shown).

Embodiment 3

[0043] 40 g of the off-white powder obtained in Example 2 was dissolved with 1 L of 50% acetonitrile aqueous solution into the upper column liquid, and introduced into UniPS40 resin for adsorption. The resin loading was 5 L, and the upper column flow rate was 5 L / h. Then use 40L of 65% acetonitrile aqueous solution to desorb, collect in sections, and mix the components with a purity of 95% or more. Concentrate the mixture in vacuo at 50-60°C until a solid precipitates out, then stop the concentration, cool to room temperature, add ethyl acetate to stir, dissolve, extract, and discard the water layer. The combined ethyl acetate layers were concentrated to dryness to obtain a white solid, which was dissolved by adding ethanol and heated to 50°C. The amount of ethanol was 12 times the weight of the white solid, and the temperature was lowered to 5°C while stirring. A white solid was precipitated, and the stirring was continued until the precipitated solid disappeared. Add more, f...

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PUM

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Abstract

The invention discloses a method for preparing high-purity fidaxomicin. Specifically, the method comprises the step of preparing the high-purity fidaxomicin by using resin chromatography and crystallization technologies. The method has the advantages that common ordinary-pressure columns are used in twice column chromatography and medium pressure is not used for preparing the chromatography, so that the previous equipment investment of the product is greatly decreased, the equipment requirement is low and the production cost is effectively reduced; the fidaxomicin is purified by using the resin adsorption and crystallization technologies, so that the operation method is simple, the yield and the purity are greatly improved, the total yield is 50-60%, and the purity is above 99%; and therefore, the method is more suitable for industrial production.

Description

technical field [0001] The invention relates to the technical field of industrial microorganisms, in particular to a method for extracting macrolide antibiotics, and more specifically, to a method for extracting fidaxomicin. Background technique [0002] Clostridium difficile infection ( Clostridium dfficile infection, CDI) is caused by an overgrowth of anaerobic Gram-positive bacilli that release toxins that can lead to colonic inflammation, severe diarrhea, and even death. [0003] Fidaxomicin is a cystic fungus produced by Actinomycetes Dactylosporangium aurantiacum subspecie hamdenensis The 18-membered ring macrolide antibiotics produced by the fermentation of NRRL 18085, also known as fidamicin and tiacumicin B, were approved by the FDA on May 27, 2011 for the treatment of Clostridium difficile (Clostridium difficile Bacillus)-associated diarrhea (CDAD). Its mechanism of action is novel, mainly through the inhibition of bacterial RNA polymerase to produce a rapid...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H17/04C07H1/06
CPCC07H1/06C07H17/04
Inventor 唐恒杨久林孟宪柱袁建栋
Owner CHONGQING QIANTAI BIOLOGICAL MEDICINE
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