Study On The Synthesis Of Linezolid

In recent years,more and more drug-resistant strains emerge,bacterial resistance development has become a very serious clinical problem for many classes of antibiotics.Because multiple drug resistance is a growing problem,physicians are now confronted with infections for which there is no effective therapy.Therefore,This growing problem of multi-drug resistance has recently rekindled interest in search for new antibiotic structural classes that inhabit or kill by novel mechanisms.Linezolid[(S)-N-[[3-[3-fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide]is marketed in the United States by Pfizer,inc,under the name ZYVOX.Linezolid inhibit synthesis of bacteria protein in early stage,on the contrary,other antibiotics inhibit in last stage.It rarely apprears cross resistance,so it is considered to be a most important antibiotic of most significant cliinical value,which is a new classical antibiotic developed after 30 years of research.In this study,N-Carbobenzoxy-3-fluoro-4-morphlinylaniline is synthesized from 3,4-difluoro-nitrobenzene and morpholine via substitution,reduction,substitution by three steps,and(s)-N-[2-(acet-yloxy)-3-chloropropyl]acetamide is synthesized from Chloromethylo-xirane and benzaldehyde,then linezolid is readily prepared by re-action of N-Carbobenzoxy-3-fluoro-4-morphlinylaniline and(s)-N-[2-(acetyloxy)-3-chloropropyl]acetamide.After careful research,I develop-e a new process,The quality of the end-product can control,whic-h Comply with the requirements of the industrialized mass product-ion.A multiple of the route of the synthesis of linezolid has been reported,the most of which has many defects,including yield,purit-y,un-convenient disposition and so more or less problematic.This p-aper mainly research the new route of the synthesis of the linezoli-d.As result,the final product from the new route has been confir-med by HPLC and H-NMR,with the total yield of 12.8%,purity 98.9%.