摘要
以5-甲基异噁唑-4-甲酸（1）为起始原料,经酰氯化得5-甲基-4-异噁唑甲酰氯（2）,2与三氟甲基苯胺（3）缩合反应,得来氟米特异构体（4）,最后经氢氧化钠水解,得水解产物5,纯度〉98%,收率为74%-85%。所合成的化合物经熔点和质谱分析确证,为来氟米特质量控制提供依据。
Leflunomide isomers 4 were synthesized by the reaction of 5-methylisoxazole-4-carboxylic acid（1）with thionyl chloride, followed by condensation with（trifluoromethyl） aniline. The title compounds 5 with 98% purity in overall yield of 74%-85% were synthesized by hydrolysis reaction with sodium hydroxide form 4. All the structures of isomers were characterized by melting point and MS spectra, which can provided datas to leflunomide quality control.
出处
《精细化工中间体》
CAS
2016年第1期46-49,共4页
Fine Chemical Intermediates
基金
台州职业技术学院2016年大学生科技创新项目(2015DKC05)
台州市海洋生物资源开发与利用科技创新团队项目(MBR2014004)
