関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Citric Acid | HCID 311 | — |
| 反応物 | Tetramethylammonium fluoride | HCID 67803 | — |
| 反応物 | 4-[2-(t-Butyldimethyl silyloxy)ethyl]-1-(6-trifluoromethyl benzothiazole-2-yl)piperidine-4-carbonitrile | HCID 57966452 | — |
| 生成物 | 4-(2-Hydroxyethyl)-1-(6-trifluoromethyl benzothiazole-2-yl)piperidine-4-carbonitrile | HCID 57966567 | 95% |
反応手順
To 4-[2-(t-butyldimethyl silyloxy)ethyl]-1-(6-trifluoromethyl benzothiazole-2-yl)piperidine-4-carbonitrile (510 mg) was added tetramethylammonium fluoride (1 M tetrahydrofuran solution, 1.63 mL). The mixture was stirred at 0° C. for 0.5 hour. To the reaction solution was added aqueous citric acid solution and extracted with ethyl acetate. The organic layer was washed with water and brine, and dried over sodium sulphate. The solvent was evaporated under reduced pressure and the residue was purified by column chromatograph on silica gel to give the title compound (366 mg). Yield: 95%.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08097610B2 |
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| 出典データセット | uspto-grants-2012_01 |
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| ORD ID | ord-3f30962b45294306898de9dec91c9712 |
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| 出典メモ | uspto-grants-2012_01 |
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