関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 4-(Trifluoromethoxy)benzenemethanol | HCID 137184 | — |
| 反応物 | ethyl 4-chloro-2-(2,3-dihydro-1H-indol-1-yl)-5-pyrimidinecarboxylate | HCID 21990788 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | ethyl 2-(2,3-dihydro-1H-indol-1-yl)-4-{[4-(trifluoromethoxy)benzyl]oxy}-5-pyrimidinecarboxylate | HCID 21990327 | 53.2% |
反応手順
To a solution of ethyl 4-chloro-2-(2,3-dihydro-1H-indol-1-yl)-5-pyrimidinecarboxylate (520 mg, 1.72 mmol) in N,N-dimethylformamide (5 mL) was added potassium carbonate (829 mg, 6 mmol) and 4-(trifluoromethoxy)benzyl alcohol (384 mg, 2 mmol) and the mixture was stirred at 100° C. for 18 h. The reaction mixture was allowed to cool to room temperature and water was added, which was followed by extraction with ethyl acetate. The organic layer was washed with saturated brine and dried over anhydrous sodium sulfate. The solvent was concentrated under reduced pressure and the residue was applied to silica gel column chromatography and eluted with hexane-ethyl acetate (4:1) to give the title compound (420 mg, 53%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07087597B1 |
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| 出典データセット | uspto-grants-2006_08 |
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| ORD ID | ord-47cbd00618f04a099dd5260bd5b784b4 |
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| 出典メモ | uspto-grants-2006_08 |
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