Qiao Jun-hua
2012
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0
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Journal
Chinese Journal of New Drugs
Abstract
Objective: To study the new process of synthesis of cefonicid sodium.Methods: 7-amino-3-[sulphomethyl-1-H-tetrazol-5-yl-thiomethy1]-3-cephem-4-carboxylic(7-AMT) was generated from synthesis reaction of 7-aminocephalosporanic acid(7-ACA) and 5-mercapto-1,2,3,4-tetrazole disodium(SMT) via 'one pot' with catalyst BF3.7-AMT and D-(-)-formylmandeloyl chloride were acylated at pH 6.5~7.0,removed formyl and generated cefonicid acid with hydrochloric acid.Cefonicid benzathine salts was generated from cefonicid acid's reaction with N,N-dibenzylethylene diamine diacetate(DBED),and then cefonicid amine salt was converted to cefonicid sodium salt by ion exchange with cation resins.Results and Conclusion: The reaction route was shortened.The overall yield of cefonicid sodium was increased to 74.5%.The route was suitable for commercial production.