T-1317, T-0901317
N-(2,2,2-三氟乙基)-N-[4-[2,2,2-三氟-1-羟基-1-(三氟甲基)乙基]苯基]-苯磺酰胺Chemical Name: N-(2,2,2-Trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]benzenesulfonamide
CAS No. 293754-55-9
项目整合开发状态: Preclinical
项目研究机构: Amgen (Originator)
合成路线:Treatment of aniline (I) with hexafluoroacetone trihydrate (II) and p-toluenesulfonic acid affords derivative (III),which is then derivatized with trifluoroacetic anhydride (IV) to provide trifluoroacetanilide derivative (V).Reduction of (V) by means of LiAlH4 in refluxing THF yields N-trifluoroethylaniline derivative (VI),which is finally converted into the target sulfonamide by reaction with benzenesulfonyl chloride (VII) in pyridine.
合成路线:The target compound is obtained by sulfonylation of aniline (I) with benzenesulfonyl chloride (II) in MeOH.
📌 参考资料/链接：
参考文献标题:Compsns.and methods for raising HDL cholesterol levels
文献作者:Shan,B.(Tularik Inc.)
参考来源:WO 0103705
📄 详细内容
合成路线:Treatment of aniline (I) with hexafluoroacetone trihydrate (II) and p-toluenesulfonic acid affords derivative (III),which is then derivatized with trifluoroacetic anhydride (IV) to provide trifluoroacetanilide derivative (V).Reduction of (V) by means of LiAlH4 in refluxing THF yields N-trifluoroethylaniline derivative (VI),which is finally converted into the target sulfonamide by reaction with benzenesulfonyl chloride (VII) in pyridine.
参考文献标题:LXR modulators
文献作者:Liu,J.; Li,L.; Cutler,S.T.; Zhu,L.; Shan,B.; Medina,J.C.; Hasegawa,H.; Lustig,K.(Tularik Inc.)
参考来源:EP 1161233; WO 0054759
产品链接: CAS No. 293754-55-9››