| 新型免疫抑制剂来氟米特合成的改进 |
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| 引用本文： | 陈卫民,徐继红.新型免疫抑制剂来氟米特合成的改进[J].南方医科大学学报,1999,19(3):256-257. |
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| 作者姓名： | 陈卫民 徐继红 |
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| 作者单位： | 第一军医大学药物研究所,广州,510515 |
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| 基金项目： | 广州市科委重点项目!97-Z－48－10 |
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| 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。
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| 关 键 词： | 来氟米特 免疫抑制剂 合成 |
Improvement of synthesis of leflunomide as immunosuppressive drug |
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| Chen Weimin,Xu Jihong.Improvement of synthesis of leflunomide as immunosuppressive drug[J].Journal of Southern Medical University,1999,19(3):256-257. |
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| Authors: | Chen Weimin Xu Jihong |
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| Abstract: | 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. |
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| Keywords: | leflunomide immunosuppressive drug synthesis |
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