ZK-230211
11beta-(4-乙酰苯基)-17β-羟基-17-(五氟乙基)estra-4,9-二烯-3-酮Chemical Name: 11beta-(4-Acetylphenyl)-17beta-hydroxy-17-(pentafluoroethyl)estra-4,9-dien-3-one
CAS No. 211254-73-8
项目整合开发状态: Phase I
项目研究机构: Jenapharm (Originator), Schering AG (Originator)
合成路线:Addition of the organolithium reagent generated from 1,1,1,2,2-pentafluoro-2-iodoethane (II) and MeLi稬iBr complex to the known ketone (I) furnished the pentafluoroethyl carbinol (III).Acid treatment of (III) with H2SO4 in methanol then removed both acetal protecting groups with concomitant dehydration of the 5-hydroxyl group to yield the title compound.
📌 参考资料/链接：
参考文献标题:Antigestagenic steroids with a fluorinated 17alpha-alkyl chain
文献作者:Schneider,M.; Cleve,A.; Neef,G.; Schwede,W.; Fuhrmann,U.; Chwalisz,K.; Hess-Stumpp,H.; Klar,U.(Schering AG)
参考来源:DE 19706061; JP 2001510479; WO 9834947
📄 详细内容
合成路线:Addition of the organolithium reagent generated from 1,1,1,2,2-pentafluoro-2-iodoethane (II) and MeLi稬iBr complex to the known ketone (I) furnished the pentafluoroethyl carbinol (III).Acid treatment of (III) with H2SO4 in methanol then removed both acetal protecting groups with concomitant dehydration of the 5-hydroxyl group to yield the title compound.
参考文献标题:Synthesis and biological activity of a novel,highly potent progresterone receptor antagonist
文献作者:Furhmann,U.; Hess-Stumpp,H.; Cleve,A.; Neef,G.; Schwede,W.; Hoffmann,J.; Fritzemeier,K.-H.; Chwalisz,K.
参考来源:J Med Chem 2000,43(26),5010
产品链接: CAS No. 211254-73-8››