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4'-(Trifluoromethyl)(1,1'-biphenyl)-2-carboxylic acid → 1-Benzyl-4-(4'-trifluoromethylbiphenyl-2-carbonylamino)piperidine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4'-(Trifluoromethyl)(1,1'-biphenyl)-2-carboxylic acid | HCID 55251 | — |
| 反応物 | 1-Benzyl-4-piperidylamine | HCID 415852 | — |
| 反応物 | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| 反応物 | 1-Hydroxybenzotriazole hydrate | HCID 2796029 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 1-Benzyl-4-(4'-trifluoromethylbiphenyl-2-carbonylamino)piperidine | HCID 22995692 | 90.7% |
反応手順
4′-Trifluoromethyl-biphenyl-carboxylic acid (5.0 g) was dissolved in dimethylformamide (50 mL), and to this solution were added at room temperature 4-amino-1-benzylpiperidine (3.55 g), 1-hydroxybenzotriazole hydrate (3.0 g) and 1-ethyl-3-(3′-dimethylaminopropyl)carbodiimide hydrochloride (3.58 g). The mixture was stirred at room temperature overnight, and the reaction solution was concentrated in vacuo to precipitate crystals. The crystals were washed successively with saturated aqueous sodium bicarbonate and water, and dried in vacuo to give the title compound (7.42 g).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07538140B2 |
| 出典データセット | uspto-grants-2009_05 |
| ORD ID | ord-a99ba96bcbe94e9f809d866deea4b699 |
| 出典メモ | uspto-grants-2009_05 |