Cephalosporin Antibiotic Cefuroxime Sodium

Cefuroxime sodium belongs to the second Cephalosporin Antibiotic. It was first developed by GlaxoSmithKline and widely used for its broad-spectrum and high stability to P-lactometers.In order to simplify the difficulty of process operation, improve the yield of Cefuroxime, reduce the cost to make it more conducive to industrial production, we studied the synthesis routes and conditions of Cefuroxime. The dissertation included three parts:In the first part, we summarized the definition, mechanism, current situation and development trend of antibiotics. Then the summarized the characteristics of Cefuroxime in detail. The preparation knowledge was necessary for our works.In the second part, the physicochemical properties and synthetic routes of Cefuroxime were discussed and its chemical structure was given. On the basis of a mass of related references and experiment research, we compared the structure of Cefuroxime and its raw materials, and then several practical synthesis routes were proposed. A feasible production process was attained. In the experiment,7-amino-cephalosporanic acid as starting material, Cefuroxime was attained by a series of chemical reactions, including hydrolysis, amidation, carbamoylation.In the third part, the synthetic route was optimized, appropriate raw material was screened and the optimum process and separation methods were determined. In the process of hydrolysis, sodium hydroxide alkaline hydrolysis method was given first priority to, and discussed the temperature, pH value, reaction time of hydrolysis. In the process of amidation, acetone was added to reduce side reaction and expand effective contact area, and chosen sodium hydroxide as the acid binding agent to promote the positive reaction. In the process of carbamoylation, chlorosulfonyl isocyanate was used as linker and a mixture of sodium lactate and sodium acetate was used to prepare Cefuroxime sodium.The overall yield was40.6%, and compared to the original route, the cost was greatly reduced. In addition, we also preliminary studied the alcoholysis in the hydrolysis and carbamoylation process, but due to the limitation of the experimental conditions and time factors, further researches were necessary.In the forth part, he major results and the prospects for the further research were reviewed.