利奈唑胺制备工艺的优化研究  

Optimization of the Preparation of Linezolid

作　　者：顾荣领 罗海荣 Gu Rongling;Luo Hairong(School of Material and Chemical Engineering,Tongren University,Tongren 554300,China;Zhejiang Hisunpharm Co.,Ltd.,Taizhou 318000,China)

机构地区：[1]铜仁学院材料与化学工程学院,贵州铜仁554300 [2]浙江海正药业股份有限公司,浙江台州318000

出　　处：《山东化工》2018年第9期13-14,21,共3页Shandong Chemical Industry

基　　金：贵州省武陵天然产物应用技术工程中心(黔教合KY字[2017]024);铜仁学院博士科研启动基金(trxy DH1605);贵州省科技合作计划项目(黔科合LH字[2016]7309号)

摘　　要：以吗啉和3,4-二氟硝基苯为原料,通过缩合、还原、环合、肼解、和酰化反应制备利奈唑胺,优化了合成工艺中还原反应和环合反应步骤:在还原反应中,用氢气还原代替甲酸铵做氢源;在环合反应中,用固体光气代替光气反应构建噁唑烷酮,并优化固体光气的反应温度对反应的影响,确定了最佳反应条件,总收率达65.2%,产品结构经~1HNMR、ESI-MS确证。With morphpline and 3,4-difluoronitrobenzene as raw material,linezolid was obtained through condensation,reduction,cyclization,hydrazinolysis,and acylation. The steps of reduction and cyclization reaction in the synthesis reaction were optimized： in the reduction,hydrogen was used as a source of ammonium formate; in cyclization reaction,triphosgene was used in place of phosgene to form oxazolidinone. The effects of material and temperature on the reaction were explored and the optimum reation conditions were determined. The total yield was 65. 2% and the product structure was determined by ^1HNMR,ESI-MS.

关 键 词：利奈唑胺 还原反应 固体光气 环合反应 

分 类 号：TQ465[化学工程—制药化工]