PROCESS DEVELOPMENT FOR SYNTHESIZING CEFPODOXIME PROXETIL

Abstract

Cephalosporins are the highly used Broad spectrum antibiotics, belong to β-lactam class . It was discovered by Brotzu in fungus Cephalosporium Acremonium which produces a chemical which show antimicrobial activity. Abraham isolated the three types of cephalosporin antibiotics cephalosporin P, cephalosporin N, cephalosporin C.7-ACA is widely used as the substrate for synthesizing cephalosporin antibiotics. Modification of the 7-ACA side-chains resulted in the development of useful antibiotic agents, and the first agent is Cephalothin (cefalotin) was launched by. Eli Lilly Company in 1964. Cephalosporins resemble penicillin in that they have a β-lactam structure, but the five-member thiazolidine ring characteristic of the penicillin is replaced by a six-member dihydrothiazine ring. The bactericidal action of beta lactam antibiotics is directly attributable to their ability to react with PBP's. The research work relates to an improved and cost effective process for the industrial manufacture of Cefpodoxime Proxetil. More specifically it relates to preparation of products of good quality with high yield and the products are removed and the same can be recycled using simple industrial and viable method. It can be possible with by using intermediate MAEM to synthesize Cefpodoxime proxetil. The drug is registered in USP and belongs to 3 rd generation drug. There are many patents which gives the procedure of Synthesis of Cefpodoxime Proxetil. These synthesis procedures have taken as standard procedure for pursuing the project work. At present, MAEM is highly used intermediate to synthesis cephalosporin antibiotics. In this project work modification has done for synthesizing of cephalosporin antibiotics by utilizing MAEM as intermediate and other chemicals like different Lewis acid, and solvent as alternate of intermediate, chemicals and solvents which are given in patents to synthesize cephalosporin antibiotics .Resulting yield has improved via making small time synthesis reaction .This is helpful for the commercial purpose. The Reaction monitoring were done by HPLC and identification of final product were done by MASS, I.R, NMR and then comparing with the well known literature. Recovery of the side product and byproduct (mercaptobenzothiazole) were achieved to allow a greener process and utilizes for synthesis of other familiar drugs.