Study On Synthesis Process Of Antibacterial Drug Linezolid

Linezolid is a novel oxazolidinone type antibiotics with remarkable therapeutic effect on treatment of infections caused by Gram-positive bacteria,which has a promising development prospect.However,due to the restriction of related patents,the sales price of linezolid is so expensive that its domestic market share is too low.Thus,it would be great challenging and significant work to develop an easily industrialized synthetic route with independent intellectual property for linezolid.By employing the commercial available dibenzylamine and(S)-epoxy chloropropane as starting materials,a simple and efficient synthetic route was developed to prepare linezolid through a serious of organic reactions with a 70%overall yield,such as epoxide ring-opening,substituted cyclization,debenzylation by hydrogenation into salt and acetylation.After the route was explored and defined,the corresponding process parameters were further optimized to seek the best reaction conditions,including catalyst type and usage,solvent,charging mode,work-up,etc.A suitable potential manufacturing process was developed.The process has the advantages of cheap and commercial available starting materials and reagents,mild reaction conditions,easily to be operated,no special equipment requirements,and low cost,which was demonstrated the developed process has a good industrial production prospect.Finally,the industrial manufacturing plan was established and confirmed based on process parameters,equipment selection and the engineering compatibility assessment between process and equipment.In addition,the quality and yields of linezolid reached the expected setting standard by conducting pilot production.