Studies On The Synthetic Process Of Cefsulodin Sodium And Prepation Of New Cephalosporin Compoumds

Cefsulodin sodium, belonging to the third-generation cephalosporin, is the frist injected anti-P.aeruginosa cephalosporin. It was exploitated by Wutian medicinal company in Japan, which was not yet reported in China. Therefore, the improvement on the synthesis process of cephalosporin sodium is a significant work. We studied the new synthesis process of cephalosporin sodium, and prepared cephalosporin sodium as well as six kinds of new compounds. The research work includes two parts shown as below:1) The novel synthesis process of cefsulodin sodium. The cephalosporin sodium was prepared from phenylacetic acid,7-ACA and pyrazinamide by 7-step reactions of sulfonation, salification, ion exchange, acylation, amidation, alkylation. Every reactive condition was studied and improved. The total yield reached 30.44%. The main intermediates and cefsulodin sodium were confirmed by IR,MS,1H-NMR.2) Though medicinal contrive software, several novel cephalosporin derivatives were designed. We improved the synthesis process in order to achieve better reactive condition, the foregoing compounds were prepared and confirmed by IR, MS.