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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
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
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| 反応物 | 3-Fluorobenzenesulfonamide | HCID 150924 | — |
| 反応物 | 3-Fluorobenzenesulfonyl Chloride | HCID 2734258 | — |
| 反応物 | Ether hydrochloride | HCID 10953452 | — |
| 反応物 | Tert-butyl 4-(3,4-diaminophenyl)-1,4-diazepane-1-carboxylate | HCID 22272464 | — |
| 反応物 | N-{2-amino-4-[4-t-butyloxycarbonyl-homopiperazin-1-yl-]phenyl}3-fluorobenzenesulfonamide | HCID 22272531 | — |
| 溶媒 | Methanol | HCID 887 | — |
| 生成物 | N-(4-(1,4-diazepan-1-yl)-2-{[(3-fluorophenyl)sulfonyl]amino}phenyl)-3-fluorobenzenesulfonamide hydrochloride | HCID 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
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07173035B2 |
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| 出典データセット | uspto-grants-2007_02 |
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| ORD ID | ord-3a95fe92913446f8b4b452cab16de588 |
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| 出典メモ | uspto-grants-2007_02 |
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