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1-Benzyl-4-(4'-trifluoromethylbiphenyl-2-carbonylamino)piperidine → N-(Piperidin-4-yl)-4'-(trifluoromethyl)-biphenyl-2-carboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1-Benzyl-4-(4'-trifluoromethylbiphenyl-2-carbonylamino)piperidine | HCID 22995692 | — |
| 触媒 | Palladium hydroxide | HCID 9942167 | — |
| 溶媒 | Tetrahydrofurfuryl alcohol | HCID 7360 | — |
| 生成物 | Ammonia | HCID 222 | — |
| 生成物 | N-(Piperidin-4-yl)-4'-(trifluoromethyl)-biphenyl-2-carboxamide | HCID 9928271 | 176.4% |
反応手順
To a solution of the 1-benzyl-4-(4′-trifluoromethylbiphenyl-2-carbonylamino)piperidine (1.47 g) obtained in Example 8a) in tetrahydrofuran-methanol (1:1; 50 mL) was added palladium hydroxide (300 mg) in a stream of argon under ice-cooling. The mixture was stirred for one day at normal pressure under hydrogen atmosphere, and further stirred for one day at normal pressure under hydrogen atmosphere after further addition of palladium hydroxide (300 mg). The reaction mixture was filtered through a Celite pad and washed with methanol. The filtrate and the washings were combined, concentrated in vacuo and purified by column chromatography on silica gel with chloroform:methanol:aqueous ammonia=100:10:1 to give the title compound (1.03 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-acf22412513b4430899df264ef800621 |
| 出典メモ | uspto-grants-2009_05 |