来氟米特的合成工艺研究  

Study on techniques for synthesis of Leflunomide

作　　者：杜会茹[1] 马东来[2] 郝六平[1] 孙威[3] 

机构地区：[1]河北化工医药职业技术学院制药工程系,河北石家庄050026 [2]河北大学化学与环境科学学院,河北保定071002 [3]中国地质科学院水文地质环境地质研究所,河北石家庄050803

出　　处：《精细与专用化学品》2011年第8期14-15,共2页Fine and Specialty Chemicals

摘　　要：以乙酰乙酸乙酯为原料,与原甲酸三乙酯、乙酸酐反应生成乙氧基衍生物,再与盐酸羟胺反应生成5-甲基-4-异噁唑甲酸甲酯,经水解、氯代后与对氟三甲基苯胺生成产物来氟米特,五步总收率29.2%。产品质量稳定,并成功的实现中试化生产。Leflunomide was synthesized using ethyl acetoacetate as starting material,which reacted with triethyl orthoformate and acetic oxide to give ethoxymethylene derivative,and then cyclization,hydrolyzed and chloride to obtain the important intermediate.Finally,this compound was converted with 4-（trifluoromethyl） aniline into Leflunomide,The total ylied of five steps was 29.2%.The product had a stabile quality,and achieved industrial manufacturing successfully.

关 键 词：来氟米特 合成 工业化 

分 类 号：TQ463.5[化学工程—制药化工]