Sulofenur, LY-186641
磺氯苯脲Chemical Name: N-(4-Chlorophenylaminocarbonyl)indane-5-sulfonamide; N-(5-Indansulsulfonyl)-N'-(4-chlorophenyl)urea
CAS No. 110311-27-8
项目整合开发状态: Phase II
项目研究机构: Lilly (Originator)
合成路线:1) 5-Indansulfonamide (I) is converted to ethyl N-(5-indansulfonyl)carbamate (II) with ethyl chloroformate and potassium carbonate in refluxing 2-butanone,which is then reacted with 4-chloroaniline (III) in toluene at reflux to provide sulofenur.2) Alternatively,(I) can be converted to its anion with NaOH in aqueous acetone,then reacted with 4-chlorophenylisocyanate (IV) to give sulofenur directly.
📌 参考资料/链接：
参考文献标题:Novel agents effective against solid tumors: The diarylsulfonylureas.Synthesis,activities and analysis of quantitative structure-activity relationships
文献作者:Grossman,C.S.; Kramer,K.E.; Crowell,T.A.; Grindey,G.B.; Rieder,B.J.; Rinzel,S.M.; Harper,R.W.; Howbert,J.J.; Tao,E.V.; Aikins,J.; Shaw,W.N.; Poore,G.A.; Todd,G.C.
参考来源:J Med Chem 1990,33(9),2393-407
📄 详细内容
合成路线:1) 5-Indansulfonamide (I) is converted to ethyl N-(5-indansulfonyl)carbamate (II) with ethyl chloroformate and potassium carbonate in refluxing 2-butanone,which is then reacted with 4-chloroaniline (III) in toluene at reflux to provide sulofenur.2) Alternatively,(I) can be converted to its anion with NaOH in aqueous acetone,then reacted with 4-chlorophenylisocyanate (IV) to give sulofenur directly.
参考文献标题:Sulofenur
文献作者:Howbert,J.J.
参考来源:Drugs Fut 1991,16(6),517
合成路线:1) 5-Indansulfonamide (I) is converted to ethyl N-(5-indansulfonyl)carbamate (II) with ethyl chloroformate and potassium carbonate in refluxing 2-butanone,which is then reacted with 4-chloroaniline (III) in toluene at reflux to provide sulofenur.2) Alternatively,(I) can be converted to its anion with NaOH in aqueous acetone,then reacted with 4-chlorophenylisocyanate (IV) to give sulofenur directly.
参考文献标题:Indentification of diarylsulfonylureas as novel anticancer drugs
文献作者:Grindey,G.B.
参考来源:Proc Amer Assoc Cancer Res 1988,29553-6
产品链接: CAS No. 110311-27-8››