関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 3-(Trifluoromethyl)benzenesulfonyl chloride | HCID 2733250 | — |
| 反応物 | 1-Benzyl-N-cyclopropylpiperidin-4-amine | HCID 2735481 | — |
| 反応物 | N-(1-benzylpiperidin-4-yl)-N-cyclopropyl-3-trifluoromethyl-benzenesulfonamide | HCID 4114155 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | N-Cyclopropyl-N-piperidin-4-yl-3-(trifluoromethyl)benzenesulfonamide | HCID 2773944 | — |
| 生成物 | N-(1-benzylpiperidin-4-yl)-N-cyclopropyl-3-trifluoromethyl-benzenesulfonamide | HCID 4114155 | — |
反応手順
N-(1-Benzylpiperidin-4-yl)-N-cyclopropyl-3-trifluoromethyl-benzenesulfonamide: N-Benzyl-4-cyclopropylaminopiperidine (5.0 g, 21.71 mmol) and triethylamine (3.6 mL, 26.05 mmol) were dissolved in dichloromethane (DCM, 100 mL). 3-Trifluoromethylbenzenesulfonyl chloride (3.47 mL, 21.71 mmol) was added and the resulting reaction mixture was stirred overnight. The mixture then was poured into potassium carbonate solution (200 mL), extracted with ether (2×200 mL), dried (MgSO4), and concentrated in vacuum to give a crude product as a yellow gum, which was purified by column chromatography on silica gel (hexane/EtOAc, 2:1). The title compound N-(1-benzylpiperidin-4-yl)-N-cyclopropyl-3-trifluoromethyl-benzenesulfonamide was obtained (9 g, 95% yield) as a pale yellow gum. Rf=0.42 (UV detection).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08937181B2 |
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| 出典データセット | uspto-grants-2015_01 |
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| ORD ID | ord-1f6641ea8fe248938efe7100e90267a5 |
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| 出典メモ | uspto-grants-2015_01 |
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