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项目整合精选>>>Teriflunomide, HMR-1726, 1726, A-771726, RS-61980, SU-0020
Teriflunomide, HMR-1726, 1726, A-771726, RS-61980, SU-0020
特立氟胺Chemical Name: (Z)-2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide
CAS No. 108605-62-5, 282716-73-8 (monosodium salt)
项目整合开发状态: Phase III
项目研究机构: Aventis Pharma (Originator), Sugen (Licensee)
合成路线:5-Methylisoxazole-4-carboxylic acid (I) was converted to the corresponding acid chloride (II) upon refluxing with SOCl2.Coupling of acid chloride (II) with 4-(trifluoromethyl)aniline (III) produced anilide (IV).Finally,isoxazole ring opening in the presence of NaOH gave rise to the title cyano amide.
📌 参考资料/链接：
参考文献标题:Isoxazole-4-carboxamides and hydroxyalkylidene-cyanoacetamides,drugs containing these cpds.and use of such drugs
文献作者:Bartlett,R.R.; K鋗merer,F.-J.(Aventis SA)
参考来源:EP 0527736; JP 1993506425; JP 1999322700; JP 1999343285; US 5494911; US 5532259; WO 9117748
📄 详细内容
合成路线:5-Methylisoxazole-4-carboxylic acid (I) was converted to the corresponding acid chloride (II) upon refluxing with SOCl2.Coupling of acid chloride (II) with 4-(trifluoromethyl)aniline (III) produced anilide (IV).Finally,isoxazole ring opening in the presence of NaOH gave rise to the title cyano amide.
参考文献标题:Immunosuppressive agents
文献作者:Coghlan,M.J.; Luly,J.R.; Wiedeman,P.E.(Abbott Laboratories Inc.)
参考来源:WO 9424095
产品链接: CAS No. 108605-62-5››