Synthetic method of cefadroxil

Abstract

The invention discloses a synthetic method of cefadroxil. The synthetic method of cefadroxil comprises the following steps of: dissolving 7-aminodesacetoxycephalosporanic acid by adopting organic base at the temperature ranging from minus 10 DEG C to minus 50 DEG C to obtain 7-aminodesacetoxycephalosporanate; carrying out reaction on HPCDane salt and pivaloyl chloride at the temperature ranging from minus 20 DEG C to minus 70 DEG C to generate mixed anhydride and carrying out condensation reaction on the mixed anhydride and 7-aminodesacetoxycephalosporanate, extracting and regulating pH value of a water layer, then separating salt and regulating pH value, and crystallizing to obtain cefadroxil. By adopting the manner, the synthetic method of cefadroxil has the advantages that a process is simple, solvate does not need to be formed in a synthetic process, crystallization can be directly carried out in water, consumption of an organic solvent is reduced, production cost is reduced, yield of cefadroxil is high, various quality indexes are qualified, pharmacopeia standards are met, and implementation of industrial production can be facilitated.

Description

technical field

[0001] The invention relates to the technical field of medicine and chemical industry, in particular to a method for synthesizing cefadroxil. Background technique

[0002] Cefadroxil is a semi-synthetic first-generation oral cephalosporin, which is a broad-spectrum oral cephalosporin antibiotic. It has a broad antibacterial spectrum, and its antibacterial activity is similar to that of cefazolin. It is also effective against penicillin-resistant staphylococci. Oral absorption is good, mainly used for urinary tract, biliary tract, and respiratory tract infections, especially suitable for children.

[0003] Now the commonly used synthesis process of cefadroxil is to use 7-ADCA as the starting raw material, through condensation with the mixed anhydride generated by hydroxydangium salt and pivaloyl chloride, hydrochloric acid hydrolysis, and the cefadroxil generated and solvent such as DMF or DMAC to form The solvate was separated and dried, and then the solvat...