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Preparation method of ceftiofur intermediate

A technology for ceftiofur and intermediates, which is applied in the field of preparation of ceftiofur intermediate cefuroxime, can solve the problems of difficult operation and high safety requirements for operators, and achieves reduced production cost, low cost and easy operability , the effect of optimizing the operating parameters

Inactive Publication Date: 2014-05-21
RINGPU TIANJIN BIOLOGICAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The advantage of this method is that the yield of the target product is high, but the use of boron trifluoride etherate and boron trifluoride gas catalysis is difficult to operate in industrial production, and has certain risks, and requires high safety requirements for operators.

Method used

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  • Preparation method of ceftiofur intermediate
  • Preparation method of ceftiofur intermediate

Examples

Experimental program
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Effect test

Embodiment 1

[0024] Add water (2000mL) into the reaction flask, add sodium hydrosulfide (615.0g), stir until completely dissolved, cool to 5°C, add furoyl chloride (250.0g) dropwise, stir for 2 hours, add hydrochloric acid to adjust the pH value to 1.0, Ethyl acetate was added for extraction, and the organic phase was separated. Add anhydrous magnesium sulfate to dry. The yellow ethyl acetate solution was obtained by suction filtration, which was set aside.

Embodiment 2

[0025] The preparation of embodiment 2 furan-2-methylthiofuroic acid

[0026] Add water (1500mL) into the reaction flask, add sodium hydrosulfide (615.0g), stir until completely dissolved, cool to 0°C, add furoyl chloride (250.0g) dropwise, stir for 2 hours, add hydrochloric acid to adjust the pH value to 1.5, Add methyl tert-butyl ether for extraction, add an equal volume of saline to the organic phase, stir for half an hour, then separate the liquids to take the organic phase. Add anhydrous magnesium sulfate to dry. The yellow methyl tert-butyl ether solution was obtained by suction filtration, which was set aside.

Embodiment 3

[0027] The preparation of embodiment 3 furan-2-methylthiofuroic acid

[0028] Add water (1000mL) into the reaction flask, add sodium hydrosulfide (307.5g), stir until completely dissolved, cool to 10°C, add furoyl chloride (250.0g) dropwise, stir for 3h, add hydrochloric acid to adjust the pH value to 1.5, Dichloroethane was added for extraction, an equal volume of saline was added to the organic phase, and after stirring for half an hour, the organic phase was obtained by liquid separation. Add anhydrous sodium sulfate to dry. Suction filtration to obtain a yellow dichloroethane solution, set aside.

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Abstract

The invention relates to preparation of a ceftiofur intermediate, namely ceftiofur acid which is a chemical raw medicine for livestock. The preparation method comprises the steps of by taking refined furan-2-methylthio furoate solution and 7-aminocephalosporanic acid as reaction substrates, adding a complexing agent into a reaction solvent, and carrying out alkali regulation by virtue of a catalytic action of a boron trifluoride compound so as to obtain the ceftiofur acid. The invention aims to provide an improved method for preparing ceftiofur acid. The improved method has the advantages of high yield and purity and low cost and is easy to operate and industrial popularization is easy to carry out.

Description

technical field [0001] The invention belongs to a synthesis method of veterinary bulk drug chemicals, and specifically refers to a preparation method of cefuroxime, an intermediate of ceftiofur. Background technique [0002] 7-Amino-3-[(2-furylcarbonyl)thiomethyl]-3-cephem-4-carboxylic acid or cefuroxime is an important intermediate in the synthesis of the third-generation cephalosporin antibiotic ceftiofur. Ceftiofur has a broad-spectrum bactericidal effect and is effective against Gram-positive and negative bacteria, including lactamase-producing strains. Ceftiofur is synthesized by condensation of cefuroxime and AE-active ester under the action of an organic base. After the reaction, it needs to be further refined. The purity of cefuroxime directly affects the quality of ceftiofur, which is a key step in the process of synthesizing ceftiofur. [0003] Cefuroxime chemical structural formula: [0004] [0005] U.S. Patent 5,387,679 (disclosed on February 7, 1995) disc...

Claims

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Application Information

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IPC IPC(8): C07D501/18C07D501/04
CPCC07D501/18C07D501/04
Inventor 赵越超王小武刘拓
Owner RINGPU TIANJIN BIOLOGICAL PHARMA
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