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4-(Trifluoromethyl)phenyl isocyanate → 1-(3-{1-(4-methoxybenzyl)-4-[2-(methylamino)pyridin-4-yl]-1H-pyrazol-3-yl}phenyl)-3-[4-(trifluoromethyl)phenyl]urea
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4-(Trifluoromethyl)phenyl isocyanate | HCID 73768 | — |
| 反応物 | Sodium | HCID 5360545 | — |
| 反応物 | 4-[3-(3-aminophenyl)-1-(4-methoxybenzyl)-1H-pyrazol-4-yl]-N-methylpyridin-2-amine | HCID 67186248 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 1-(3-{1-(4-methoxybenzyl)-4-[2-(methylamino)pyridin-4-yl]-1H-pyrazol-3-yl}phenyl)-3-[4-(trifluoromethyl)phenyl]urea | HCID 67184323 | 63% |
反応手順
250 mg (0.65 mmol) of 4-[3-(3-aminophenyl)-1-(4-methoxybenzyl)-1H-pyrazol-4-yl]-N-methylpyridin-2-amine were dissolved in 10 ml of dry dimethylformamide and 92 μl of p-trifluoromethyl-phenylisocyanate were added. The reaction was stirred at room temperature overnight, poured into aqueous sodium hydrogenocarbonate and extracted with dichloromethane. The organic phase was then dried over sodium sulphate and evaporated. The residue was purified by flash-chromatography on a silica gel column CH2C12-CH3COCH3; from 9/1 to 8/2), giving 234 mg (63%) of the title compound.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08541575B2 |
| 出典データセット | uspto-grants-2013_09 |
| ORD ID | ord-156ace3574a8420d9fecbb93f87a9ee7 |
| 出典メモ | uspto-grants-2013_09 |