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Improved method for preparing ceftiofur

A technology of ceftiofur and furyl carbonyl, which is applied in the field of preparation of ceftiofur, can solve problems such as resistance to popularization, inapplicability to large-scale industrial production, unfavorable stirring crystallization, etc., and achieves low cost, high purity and easy operation Effect

Inactive Publication Date: 2012-07-18
QINGDAO UNIV OF SCI & TECH
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  • Description
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Problems solved by technology

[0004] The disadvantage of the above method is that it needs to undergo decompression concentration under high vacuum in the middle, which increases the difficulty of industrial production. At the same time, the remaining concentrate after evaporation adheres to the bottle wall, which is not conducive to stirring and crystallization. This process is not suitable for large-scale Industrialized production, which brings resistance to product promotion

Method used

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Effect test

Embodiment

[0018] Add 5.0g of 7-amino-3-[2-(furylcarbonyl)thiomethyl]-3-cephem-4-carboxylic acid to 50ml of dichloromethane and 10ml of n-butanol solution, then add 5ml of triethylamine To carry out the reaction, adjust the temperature of the system to -6~-4°C, add 6.0g of 2-methoxyimino-2-(2-amino-4-thiazolyl)-(z)-benzothiazolyl thioacetate to react 4 Hours, after the reaction finishes, add 25ml of tap water to extract, the aqueous phase is back-extracted with 80ml of methyl acetate and acetonitrile mixed solvent (volume ratio of methyl acetate and acetonitrile) 80ml, and the organic phase obtained is extracted with 10% chlorine 30ml of sodium chloride solution was processed, 30ml of distilled water was added to the organic phase, then the pH of the system was adjusted to 7-8 by sodium bicarbonate, the pH of the aqueous phase was adjusted to 3-4 with acetic acid, ceftiofur was obtained by filtration and separation, and the yield was 64.5 %, HPLC purity is 99.6%.

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Abstract

The invention relates to an improved method for preparing ceftiofur. The method comprises the following steps of: adding 7-amino-3-[2-(furylcarbonyl)thiomethyl]-3-cephem-4-carboxylic acid into a solvent system, adding triethylamine and reacting for 30 minutes; regulating the temperature of the system, adding 2-methoxyimino-2-(2-amino-4-thiazolyl)-(z)-thioacetic acid benzothiazole ester and reacting for 4 hours; adding tap water for extracting after reaction is finished, performing back extraction on a water phase by using a mixed solvent, treating the obtained organic phase by using a 10 percent sodium chloride solution, and adding distilled water into the organic phase; and regulating the pH of the system to 7-8 by using sodium bicarbonate, regulating the pH of the water phase to 3-4 by using acetic acid, filtering, and separating to obtain the ceftiofur. The yield of the ceftiofur prepared by the method is 64.5 percent, and the purity of the ceftiofur is 99.6 percent (high performance liquid chromatography HPLC).

Description

technical field [0001] The invention relates to a preparation method of medicinal chemicals, in particular to an improved preparation method of ceftiofur. Background technique [0002] Ceftiofur, chemical name 7-[2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetamido]-3-[(2-furancarbonyl)sulfur Substitute methyl]-2-cefonoic acid. Ceftiofur sodium is a cephalosporin veterinary drug developed by Pharmacia Upjohn in the 1980s. Its mechanism of action is to act on bacterial transpeptidase to block the synthesis of cell wall, presenting a bactericidal effect, and is used to treat and control bacterial intestinal and respiratory infections in livestock. Ceftiofur is a precursor substance for the production of ceftiofur hydrochloride or ceftiofur sodium, and it can also be used alone as a product. [0003] US Patent US2006 / 0149054A1 describes a preparation method of ceftiofur. The main reaction step is the use of 7-amino-3-[2-(furylcarbonyl)thiomethyl]-3-cephem-4-carboxylic aci...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/36C07D501/06C07D501/12
Inventor 吴汝林王繁业
Owner QINGDAO UNIV OF SCI & TECH
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