新产品编号:2234293
Chemical Name: N-[4-(3,20-Dioxopregn-4-en-7alpha-ylsulfanyl)phenyl]-N'-[1(R)-phenylethyl]urea
项目整合开发状态: Biological Testing
项目研究机构: Georgetown University (Originator)
合成路线:Progesterone (I) was oxidized to the 6-dehydro derivative (II) using 2,3-dichloro-5,6-dicyano-1,4-benzoquinone.Conjugate addition of 4-aminothiophenol (III) to dienone (II) furnished the aminophenyl sulfide (IV).The target urea was then obtained by coupling of the amino compound (IV) with (R)-alpha-methylbenzyl isocyanate (V).
📌 参考资料/链接：
参考文献标题:Progesterone analogs to reverse multidrug resistance
文献作者:Clarke,R.; Talebian,A.H.; Ghiorghis,A.; Leonessa,F.; Hammer,C.(Georgetown University)
参考来源:WO 9700683
📄 详细内容
合成路线:Progesterone (I) was oxidized to the 6-dehydro derivative (II) using 2,3-dichloro-5,6-dicyano-1,4-benzoquinone.Conjugate addition of 4-aminothiophenol (III) to dienone (II) furnished the aminophenyl sulfide (IV).The target urea was then obtained by coupling of the amino compound (IV) with (R)-alpha-methylbenzyl isocyanate (V).
参考文献标题:C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump
文献作者:Leonessa,F.; Kim,J.-H.; Ghiorghis,A.; Kulawiec,R.J.; Clarke,R.; Talebian,A.; Hammer,C.
参考来源:J Med Chem 2002,45(2),390