Study On Synthesis Of Cefozopran Hydrochloride

Cefozopran hydrochloride is one of the fourth-generation cephalosprins,was developed by Takeda company.It has a better antibacterial effect togram-positive bacteria and gram-negative bacteria. Its antibiotic mechanism, pharmacokinetic character, pharmacological properties, clinical effects and related synthetic methods introduced briefly in this paper.The synthetic process of cefozopran hydrochloride was researched, we researched each step of the synthetic process for the goal of improving yield, simplifying operationprocedure and cost-cut and determined the best route.Cefozopran hydrochloride is synthesized from 7-ACA, with the process of carboxyl protection, amino protection, displacement reaction, then deprotection to obtain the key intermediate 7-ACP, with AE-active ester condensation reaction, salt cefozopran hydrochloride, the yield was 27.2%.We chose dichloromethane as the solvent of one-pot procedure of preparing 7-ACP which was the key intermediate of hydrochloric cefozopran in an overall yield of27.2% scarcely with undesirable byproduct isomer. The produre was simple, mild,environment-friendly, and suitable for scale-up production.We designed also a new produre for the synthesis of hydrochloric cefozopran and obtained crude product in good yield. But it was dark-colored and need to be futher optimized.Using triethylamine catalyze to synthesis cefozopran, salt cefozopran hydrochloride.The process was easy to operate and the final product yield was improved compared with the literature.The structure of cefozopran hydrochloride was confirmed by IR,MS, 1H NMR, 13 C NMR.