SB-357134
N-(2,5-二溴铄-3-氟苯基)-4-甲氧基-3-(1-哌嗪基)苯磺酰胺Chemical Name: N-(2,5-Dibromo-3-fluorophenyl)-4-methoxy-3-(1-piperazinyl)benzenesulfonamide
CAS No. 219963-52-7
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator)
合成路线:1-(2-Methoxyphenyl)-4-trichloroacetylpiperazine (II),prepared from 1-(2-methoxyphenyl)piperazine (I) and trichloroacetyl chloride,was treated with chlorosulfonic acid to give the sulfonyl chloride (III).Coupling of chloride (III) with 2,5-dibromo-3-fluoroaniline (IV) afforded sulfonamide (IV).Finally,removal of the trichloroacetyl protecting group under basic conditions provided the title piperazine derivative.
📌 参考资料/链接：
参考文献标题:Novel cpds.
文献作者:Moss,S.F.; Bromidge,S.M.(SmithKline Beecham plc)
参考来源:WO 9902502
📄 详细内容
合成路线:1-(2-Methoxyphenyl)-4-trichloroacetylpiperazine (II),prepared from 1-(2-methoxyphenyl)piperazine (I) and trichloroacetyl chloride,was treated with chlorosulfonic acid to give the sulfonyl chloride (III).Coupling of chloride (III) with 2,5-dibromo-3-fluoroaniline (IV) afforded sulfonamide (IV).Finally,removal of the trichloroacetyl protecting group under basic conditions provided the title piperazine derivative.
参考文献标题:Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: Identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134)
文献作者:Bromidge,S.M.; Clarke,S.E.; Gager,T.; Griffith,K.; Jeffrey,P.; Jennings,A.J.; Joiner,G.F.; King,F.D.; Lovell,P.J.; Moss,S.F.; Newman,H.; Riley,G.; Rogers,D.; Routledge,C.; Serafinowska,H.; Smith,D.R.
参考来源:Bioorg Med Chem Lett 2001,11(1),55
产品链接: CAS No. 219963-52-7››