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HRID 346741作成日:2026年10月26日

3-Fluorobenzenesulfonamide → N-(4-(1,4-diazepan-1-yl)-2-{[(3-fluorophenyl)sulfonyl]amino}phenyl)-3-fluorobenzenesulfonamide hydrochloride

https://huagongshe.com/reaction/346741

反応式

関与物質

役割名称HCID仕込み量
反応物3-FluorobenzenesulfonamideHCID 150924—
反応物3-Fluorobenzenesulfonyl ChlorideHCID 2734258—
反応物Ether hydrochlorideHCID 10953452—
反応物Tert-butyl 4-(3,4-diaminophenyl)-1,4-diazepane-1-carboxylateHCID 22272464—
反応物N-{2-amino-4-[4-t-butyloxycarbonyl-homopiperazin-1-yl-]phenyl}3-fluorobenzenesulfonamideHCID 22272531—
溶媒MethanolHCID 887—
生成物N-(4-(1,4-diazepan-1-yl)-2-{[(3-fluorophenyl)sulfonyl]amino}phenyl)-3-fluorobenzenesulfonamide hydrochlorideHCID 10209725—

反応手順

The compound was prepared from 2-amino-5-(4-t-butyloxycarbonyl-1-homopiperazinyl)aniline and 3-flourobenzenesulfonyl chloride. Purification by column chromatography (CH2Cl2/MeOH/heptane, 4:1:15) gave a mixture of N-{2-amino-4-[4-t-butyloxycarbonyl-homopiperazin-1-yl-]phenyl}3fluorobenzenesulfonamide and N-{4-[4-t-butyloxycarbonyl] homopiperazinyl)-2-[(3-flourophenylsulfonyl)amino]phenyl}-3-fluorobenzenesulfonamide (0.180 g, 73%). Boc-deprotection was achieved by dissolving the mixture in small amount of MeOH and adding HCl/ether. The mixture was let at r.t. for 0.5 h. Purification by preparative HPLC gave N-(4-(1,4-diazepan-1-yl)-2-{[(3-fluorophenyl)sulfonyl]amino}phenyl)-3-fluorobenzenesulfonamide hydrochloride Anal. (C23H27ClN4O4S2) C, H, N, S.; M+524.4 Calcd 522.12.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07173035B2
出典データセットuspto-grants-2007_02
ORD IDord-3a95fe92913446f8b4b452cab16de588
出典メモuspto-grants-2007_02