FK-778, HMR-1715, X-920715, MNA-715
Chemical Name: 2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]hepta-2-en-6-ynamide
CAS No. 152418-67-2
项目整合开发状态: Phase II
项目研究机构: Aventis Pharma (Originator), Fujisawa (Licensee)
合成路线: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 ?8 C to give N-(4-trifluoromethylphenyl)-5-(3-butynyl)isoxazole-4-carboxamide (III),which is finally treated with water at 0 C.
📌 参考资料/链接：
参考文献标题:Cyano-2-hydroxy-3-enamide derivs.,process for their preparation,their use as drugs,pharmaceutical compsns.containing them and intermediates obtained
文献作者:Bartlett,R.R.; Kay,D.P.; Kuo,E.A.; Schleyerbach,R.; Schwab,W.(Aventis Pharma SA)
参考来源:EP 0551230; JP 1993310672; US 5308865
📄 详细内容
合成路线: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 ?8 C to give N-(4-trifluoromethylphenyl)-5-(3-butynyl)isoxazole-4-carboxamide (III),which is finally treated with water at 0 C.
参考文献标题:Leflunomide < Rec INN >
文献作者:Graul,A.; Castar,J.
参考来源:Drugs Fut 1998,23(8),827
合成路线: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 ?8 C to give N-(4-trifluoromethylphenyl)-5-(3-butynyl)isoxazole-4-carboxamide (III),which is finally treated with water at 0 C.
参考文献标题:FK-778
文献作者:Cullell-Young,M.; Castar,R.M.; Leeson,P.A.
参考来源:Drugs Fut 2002,27(8),733