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Preparation method of cephem carboxylate

A technology of cephem carboxylate and cephem, which is applied in the field of preparation of cephem carboxylate, can solve the problems of insufficient solubility of cephem and inability to inject, and achieve the effect of broad-spectrum antibacterial activity and high solubility

Inactive Publication Date: 2014-05-14
WUXI VISION PRO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there are various preparation methods of cephems, but the solubility of the prepared cephems in water is not enough and cannot be effectively used for injection

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] A preparation method of cephem carboxylate, said method comprising:

[0017] Under ice-cooling, 1.42g of 7β-amino-3-[4-(1-methyl-4-pyridinium)-2-thiazolylthio]-3-caproene-4-carboxylate hydrochloride The pH of the solution in a mixture of 50 ml THF and 50 ml water was adjusted to 7.4 with 12 ml of 0.6M sodium bicarbonate. Add 3.41 g of 2-(5-dichlorophosphoramido-1,2,4-thiadiazol-3-yl)-2(Z)-fluoromethoxyiminoacetyl chloride in batches to the solution, and the mixture Stir at 5°C for 10 minutes while maintaining the pH at 7.2 to 7.5 by adding 24 ml of 0.6M sodium bicarbonate. A concentrated solution of 787 mg of sodium acetate in 20 ml of water was poured into the reaction mixture, and the resulting mixture was stirred at room temperature for 3 hours. After the pH of the mixture was adjusted to 3.0 with 3.4 ml of 1N hydrochloric acid, the reaction mixture was concentrated under reduced pressure. The concentrate was diluted with 750 ml of water, and purified by MCI gel H...

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PUM

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Abstract

The invention discloses a preparation method of cephem carboxylate. The prepared cephem carboxylate has excellent antibacterial activity on gram negative bacteria and gram positive bacteria which include staphylococcus aureus and MRSA (Methicillin Resistant Staphylococcus Aureus) and is used for curing and preventing the infectious diseases caused by the gram negative bacteria and the gram positive bacteria. A cephem compound has rather high solubility in water, thereby being favourably used for injection.

Description

technical field [0001] The invention relates to a preparation method of medicine, in particular to a preparation method of cephem carboxylate. Background technique [0002] Cephalosporin is the general term for cephalosporin antibiotics. Cephalosporins (Cephalosporins) is a class of antibiotics obtained by semi-synthetic modification of the side chain of natural cephalosporin C obtained from the culture of Cephalosporus coronaris. [0003] In the antibiotic market, cephalosporin antibiotics occupy a larger share, and their related intermediates also show considerable market potential. Among the cephalosporin antibiotics, the most sold varieties include ceftriaxone sodium, cefazolin sodium, cefotaxime, ceftriaxone, cefoperazone and cefuroxime (ester), and the corresponding intermediates include 7-ACA, 7- ADCA, GCLE, aminothioxamic acid, AE-active ester, triazine ring, tetrazolium acetic acid, methylmercaptotetrazolium, HO-EPCP, methoxyamine hydrochloride, furanamine salt (S...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6561A61P31/04
Inventor 廖秀高
Owner WUXI VISION PRO
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