189345-52-6Relevant articles and documents
A method for preparing cephalosporin lorraine ester
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, (2017/08/25)
The invention relates to a synthetic method for ceftaroline fosamil. According to the synthetic method, 7-phenylacetamide-3-hydroxy-3-cephalosporin-4-carboxylate-diphenylmethyl is selected as a raw material to be chloridized and reacts with 4-(4-pyridyl)-1,3-thiazole-2-thiol sodium salt at a C-3 site to obtain a thioether compound, p-cresol and immobilized penicillinase are adopted for removing carboxyl and amino protecting groups respectively, the thioether compound and the acylated AE-active ester are subjected to C-7 site condensation reaction, and crystallization in acetic acid is performed after hydrolyzation to prepare the ceftaroline fosamil successfully. The preparation method has the advantages that use of toxic and harmful substances such as trifluoroacetic acid and phosphorus pentachloride is avoided, reaction conditions are moderate, side reactions are few, technology is simple, yield and product purity are high, cost is low, raw materials are cheap and easy to obtain, and the preparation method is applicable to industrial production.