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【结 构 式】 
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【药物名称】FK-778, HMR-1715, X-920715, MNA-715 【化学名称】2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]hepta-2-en-6-ynamide 【CA登记号】152418-67-2 【 分 子 式 】C15H11F3N2O2 【 分 子 量 】308.26232 |
【开发单位】Aventis Pharma (Originator), Fujisawa (Licensee) 【药理作用】IMMUNOMODULATING AGENTS, Immunosuppressants, Treatment of Transplant Rejection, Dihydroorotate Dehydrogenase Inhibitors |
合成路线1
FK-778 is obtained by selective alkylation of leflunomide (I) at the methyl group with propargyl iodide (II) by means of butyl lithium in THF at 78 C to give N-(4-trifluoromethylphenyl)-5-(3-butynyl)isoxazole-4-carboxamide (III), which is finally treated with water at 0 C.
| 【3】 Bartlett, R.R.; Kay, D.P.; Kuo, E.A.; Schleyerbach, R.; Schwab, W. (Aventis Pharma SA); Cyano-2-hydroxy-3-enamide derivs., process for their preparation, their use as drugs, pharmaceutical compsns. containing them and intermediates obtained. EP 0551230; JP 1993310672; US 5308865 . |
| 【1】 Cullell-Young, M.; Castaner, R.M.; Leeson, P.A.; FK-778. Drugs Fut 2002, 27, 8, 733. |
| 【2】 Graul, A.; Castaner, J.; Leflunomide < Rec INN >. Drugs Fut 1998, 23, 8, 827. |
Extended Information