Synthesis Research For The Fourth Generation Cephalosporin Of Cefepime

Cefepime hydrochloride is the prototypical fourth-generationcephalosporin. It is firstly launched in Sweden (1993) as Maxipime byBristol-Myers Squibb for the treatment of respiratory and urinary tract,intraabdominal and skin and soft tissue infections, Septicemia/bacteremia and febrile episodes in neutropenic patients. It is suppliedas vials, 0.5,1 and 2g.The target in the present work was to study the new designed synthesismethods for the drug, to avoid the disadvantage of the literature'smethods, and to establish a technique of manufacture foundation suitablefor the situation of our country.In this paper, a novel method for conversion of ACLE to cefepimehydrochloride via inner salt(17) intermediate is presented, it is simple,easy to control, and desired product is in high quality. It is significantfor industrial production.The new designed synthesis way for cefepime is creative, not relativeliterature is reported.What is concluded are:In this paper, it is successfully completed the design of newsynthesis way for cefepime, it is proved practical, easy to control andsimple to operate, the quality of the product is high;It is prepared inoverall yields of 26% from ACLE.After analyzing the synthesis ways for cefepime exist in literature,by the new designed way, we get these results:1) discard the solvent Fron and CCl4 which is a disadvantage forenvironment protection2) avoid the restrict needing free of water, which is a disadvantage forindustrial producton.3) Discard the regents TMSI which is not easy to store and NaI which isexpensiveBy the new designed methods, after getting the product in 5L scale,it is found the quality fit the needs of applying for approval, and hasused for the applying for research in clinic.The new designed method of cefepime has established a foundation forthe production made in our country.