摘要
目的合成新型免疫抑制剂来氟米特。方法以乙酰乙酸乙酯为原料与N，N-二甲基甲酰胺二甲基缩醛反应，所得产物同盐酸羟胺反应合成5-甲基-4-异唑甲酸乙酯；后者经水解、酰氯化，与对三氯甲基苯胺反应合成出来氟米特。结果所得产品结构均经IR、HNMR、MS等光谱鉴定。
Objective To synthesize the new immunosuppressive drug, Leflunomide. Methods Reaction of ethyl acetoacetate withN,N-dimethylfomamide dimethyl acetal gave ethyl 2-dimethylaminomethyleneacetoac- which reacted with hydroxylaminehydrochloride to afford 5 - methyl-4- isoxazolecarboxylate. The ester was hydrolyzed to the corresponding carboxylic acid whichreacted with thionyl chloride to yield 5-methyl-4-isoxazolecarboxylic acid chloride. Final reaction of the acid chloride with p trifluoromethylaniline produced the Leflunomide. Results The structUres of the products were identified by IR, HNMR,MS.
出处
《第一军医大学学报》
CSCD
1999年第3期256-257,共2页
Journal of First Military Medical University
基金
广州市科委重点项目!97-Z-48-10
关键词
来氟米特
免疫抑制剂
合成
leflunomide, immunosuppressive drug, synthesis
