Process Optimization Of Linezolid And Its Analogues

The treatment of bacterial diseases is facing a growing crisis due to the emergence of multidrug-resistant bacteria.Since linezolid was put on the market,we have important implications for the study of its synthesis and the pharmacological study of analogues due to its efficacy against gram-positive pathogens and the extremely bright prospects of linezolid in the treatment of bacterial resistance.In this paper,the synthesis process of linezolid is systematically investigated,and a route more suitable for industrial production is selected for in-depth research and optimization after comprehensive consideration of the yield,economy and impurities of the process.Using cheap 3-fluoro-4-(4-morpholino)aniline and(S)-epichlorohydrin as raw materials,the final product is obtained by substitution,reduction,acylation and condensation in 4 steps.By exploring each step of the synthesis process and analyzing the process that each impurity may produce,the impurities can be better controlled in the optimization process,so as to obtain a route suitable for industrial production with high yield,less impurities,green environmental protection,mild reaction conditions,simple follow-up treatment,short steps and step-by-step,which provides reliable data for the next step of linezolid optimization production.Secondly,linezolid,as the first oxazolidinone drug applied in clinical practice,is widely used in the treatment of various drug-resistant staphylococcus aureus infections,and with the widespread use of clinical practice,the structure of linezolid has attracted widespread attention.In this paper,the one-step and two-step synthesis of linezolid analogues is explored,which not only provides preliminary basic research data for the study of the relationship between linezolid efficacy changes and structure,but also explores the one-step and two-step processes,providing an efficient method for the synthesis of lactams.