Cefixime compound and novel preparation method thereof

Abstract

The invention relates to a cefixime compound and a novel preparation method thereof. The invention point is that: by adopting pentafluorophenol as an active agent, the cefixime compound and the novel preparation method thereof have the advantages of high reaction stability, mild reaction condition, high product yield and purity, and are suitable for industrialized mass production.

Description

technical field The invention relates to a cefixime compound and a new preparation method thereof, belonging to the technical field of medicine. Background technique Cefixime, its chemical name is: (6R, 7R)-7[(Z)-2-(2-amino-4-thiazolyl)-2-(carboxymethoxyaminoimine)acetamido]-3 -Ethylene-8-oxo-5-thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylic acid trihydrate, molecular formula: C 16 h 15 N 5 o 7 S 2 ·3H 2 O, molecular weight: 507.50, structural formula: Cefixime is a third-generation oral cephalosporin with a broad antibacterial spectrum. Bacteriaceae bacteria have good antibacterial activity, are highly stable to β-lactamase, and have high affinity with penicillin-binding protein 3, 1a and 1b, which hinders the synthesis of bacterial cell walls, and the bacteria rapidly dissolve and die. Clinically, it is mostly used to treat pharyngitis, tonsillitis, acute bronchitis and acute exacerbation of chronic bronchitis, otitis media, urinary tract infection, simple gonorrhe...

AI Technical Summary

Problems solved by technology

Another advantage of the present invention is that the activation of (Z)-2-(2-aminothiazol-4-yl)-2-(methoxycarbonylmethoxy-imino)acetic acid in the present invention uses pentafluorophenol As an activator, a new cefixime active ester intermediate is obtained, which avoids the strict restrictions on anhydrous conditions caused by the use of phosphorus pentachloride and thionyl chloride, as well as the pollution caused to the environment and the impact on industrialization. The difficulty of using 2-mercaptobenzimidazole activated ester to avoid the trouble caused by the post-reaction treatment and the new impurities brought in will affect the purity of the final product; solve the problem that mercaptobenzothiazole cannot be well recovered in the original process , improve product yield and finished product quality

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