Study On The Synthetic Process Of Cefixime

Cefixime is the third generation semisynthetic cephalosporin for oral use which exerts for its antibiotic action by inhibiting the synthsis of the bacterium cell wall, It has great inhibition on both gram positive bacteria and gram negative bacteria,This antibiotic is hig hly stable to beta-lactamases, cefixime is widely used in clinical.. Some improvements of synthetic methods about cefixime are researched,mainly includes the following works.First part: The synthesis of 2-(2-aminothiazol-4-y1)-2-[[(Z)- (tert-butoxy carbonyl) methoxy]imino] acetic acid was studied,It was prepared from ethyl (Z) -2- hydroxyl -imino-2-(2-aminothiazol-4-yl) acetate via saponification, etherification and purification. The synthesis of 2-(2-aminothiazol-4-y1)-2-[[(Z)- (tert-butoxy carbonyl) methoxy]imino] acetic acid-2-S-mercaptobenzo-thiazolylester was researched. Condensate 2-(2- -aminothiazol-4-yl) - 2- [[(Z) (tert. butyoxy) carbonyloxy]imino]acetic acid with DM in presense of triethyl phosphate and triethylamine to get the target compound.cefixime was parapered from 7- amino -3- vinyclepalosperianic acid and 2-(2-aminothiazol-4-y1) -2-[[(Z)- (tert- butoxycarbonyl)methoxy]imino] acetic acid-2-S-mercaptobenzo- thiazolyl ester via amidation and hydrolysis,the total yield was 75 per.Second part:The synthesis of 2-(2-aminothiazol-4-yl)-2-[[(Z)(methoxycarbonyl) -methoxy]imino] acetic acid-2-S-mercaptobenzothiazolylester was researched.Condensate 2-(2-aminothiazol-4-yl)-2-[[(methoxycarbonyl) methoxy]imino]-acetic acid with DM in presnce of tripenylphosphine to form the target conpound. Cefixime was synthesized from 7-amino-3-vinyclepalosperi- anic acid and 2-(2-aminothiazol-4-yl)-2-[[(Z) (methoxy carb -onyl)methoxy] imino]acetic acid -2-S-mercaptobenzo-thiazolylester via amidiation and hydrolysis, the total yield was 80 per.Part three:Comparison of these two synthetic route of cefixime, An easier,lower cost and more prone to industrialization way was identified.On the base of literatures,the synthetic route of cefixime was optimized and improved.The products can be obtained in high purity and good yield in above process.As a result ,this process provides highly pure cefixime trihydrate in good yield and conven–ience for production.