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(Trifluoromethyl)trimethylsilane → 2-(Pyrrolidin-1-yl)-5-(2,2,2-trifluoro-1-hydroxyethyl)-pyridine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | (Trifluoromethyl)trimethylsilane | HCID 552549 | — |
| 反応物 | Tetrabutylammonium Fluoride | HCID 2724141 | — |
| 反応物 | 6-(Pyrrolidin-1-yl)pyridine-3-carbaldehyde | HCID 2794775 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 2-(Pyrrolidin-1-yl)-5-(2,2,2-trifluoro-1-hydroxyethyl)-pyridine | HCID 67401736 | 94% |
反応手順
According to Reference Example 8-12, by use of 6-(pyrrolidin-1-yl)-3-pyridinecarboxaldehyde (173 mg, 0.982 mmol), (trifluoromethyl)trimethylsilane (174 μL, 1.18 mmol), tetrabutylammonium fluoride (a 1.0 mol/L solution in tetrahydrofuran, 98.0 μL, 0.098 mmol) and tetrahydrofuran (5.0 mL), the mixture was stirred and reacted at room temperature for 30 minutes. Then, slurry purification was performed using hexane, to give 2-(pyrrolidin-1-yl)-5-(2,2,2-trifluoro-1-hydroxyethyl)-pyridine (Compound DH) (227 mg, yield: 94%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08673908B2 |
| 出典データセット | uspto-grants-2014_03 |
| ORD ID | ord-fd9eef4168e448158e86ec565aff527f |
| 出典メモ | uspto-grants-2014_03 |