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Indisulam, E-7070, ER-35744

N-(3-氯-1H-吲哚-7-基)-1,4-苯二磺酰胺Chemical Name: N-(3-Chloroindol-7-yl)benzene-1,4-disulfonamide
CAS No. 165668-41-7
项目整合开发状态: Phase II
项目研究机构: Eisai (Originator), Abbott (Licensee)
合成路线:The reaction of 7-nitro-1H-indole (I) with NCS in acetonitrile gives 3-chloro-7-nitro-1H-indole (II),which is reduced with Fe and NH4Cl or stannous chloride in ethanol/aq.HCl to yield 3-chloro-1H-indol-7-amine (III).Finally,this compound is condensed with 4-sulfamoylbenzenesulfonyl chloride (IV) in pyridine to afford the target sulfonamide.The intermediate 4-sulfamoylbenzenesulfonyl chloride (IV) is obtained by diazotation of 4-aminobenzenesulfonamide (V) with NaNo2 and HCl,followed by treatment with SO2 and CuCl2.
📌 参考资料/链接:
参考文献标题:Bicyclic heterocyclic sulfonamide and sulfonic ester derivs.
文献作者:Yoshino,H.; Yamato,T.; Okauchi,T.; Yoshimatsu,K.; Sugi,N.; Nagasu,T.; Ozawa,Y.; Koyanagi,N.; Kito,K.(Eisai Co.,Ltd.)
参考来源:EP 0673937; US 5721246; WO 9507276

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产品链接: CAS No. 165668-41-7››