| The development of β-lactam antibiotics and cephalosporins were briefly described in this paper, and the third-generation cephalosporin cefoperazone sodium was also introduced. The synthesis of cefoperazone sodium were studied. A new synthetic route was designed and the method was modified, which make easier to process, and the yield was elevated. The product has high purity and good crystallization. During the synthesis of the intermediate 7-ACT, green solvent-dimethyl carboxate was used and lower the cost price and decrease the pollution. The total yield was 55.08%, which was synthesized from 7-ACA by ten steps, including the preparation of side chains. Its structure was confirmed by IR, 1H-NMR, 13C-NMR and MS. |