[125I]-SB-258585
盐酸4-碘-N-[4-甲氧基-3-(4-甲基-1-哌嗪)苯基]苯磺酰胺Chemical Name: 4-[125I]Iodo-N-[3-methoxy-4-(4-methylpiperazin-1-yl)phenyl]benzenesulfonamide
CAS No. 209480-63-7 (non-labeled)
项目整合开发状态: Biological Testing
项目研究机构: GlaxoSmithKline (Originator)
合成路线:Nitration of 1-(2-methoxyphenyl)piperazine (I) using KNO3 in H2SO4 gave (II).After protection of (II) as the N-Boc derivative (III),reduction of the nitro group by catalytic hydrogenation over Pd/C yielded aniline (IV).This was condensed with 5-chloro-3-methylbenzothiophene-2-sulfonyl chloride (V) to afford the corresponding sulfonamide (VI).Finally,the Boc protecting group of (VI) was removed with HCl in boiling THF.
合成路线:The title sulfonamide was prepared by coupling 4-methoxy-3-(4-methylpiperazin-1-yl)aniline (II) with 4-iodobenzenesulfonyl chloride (I) in acetone.
📌 参考资料/链接：
参考文献标题:Sulphonamide derivs.,process for their preparation,and their use as medicaments
文献作者:King,F.D.; Bromidge,S.M.; Wyman,P.A.(SmithKline Beecham plc)
参考来源:WO 9827081
📄 详细内容
合成路线:Nitration of 1-(2-methoxyphenyl)piperazine (I) using KNO3 in H2SO4 gave (II).After protection of (II) as the N-Boc derivative (III),reduction of the nitro group by catalytic hydrogenation over Pd/C yielded aniline (IV).This was condensed with 5-chloro-3-methylbenzothiophene-2-sulfonyl chloride (V) to afford the corresponding sulfonamide (VI).Finally,the Boc protecting group of (VI) was removed with HCl in boiling THF.
合成路线:The title sulfonamide was prepared by coupling 4-methoxy-3-(4-methylpiperazin-1-yl)aniline (II) with 4-iodobenzenesulfonyl chloride (I) in acetone.
参考文献标题:5-Chloro-N-(4-methoxy-3-piperazin-1-ylphenyl)-3-methyl-2-benzothiophenesulfonamide (SB-271046): A potent,selective,and orally bioavailable 5-HT6 receptor antagonist
文献作者:Bromidge,S.M.; Brown,A.M.; Clarke,S.E.; Dodgson,K.; Gager,T.; Grassam,H.L.; Jeffrey,P.M.; Joiner,G.F.; King,F.D.; Middlemiss,D.N.; Moss,S.F.; Newman,H.; Riley,G.; Routledge,C.; Wyman,P.
参考来源:J Med Chem 1999,42(2),202
产品链接: CAS No. 209480-63-7››