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Triphenylphosphine → 2-[1-(4-Pyridyl)piperidin-4-ylmethoxy]aniline
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triphenylphosphine | HCID 11776 | — |
| 反応物 | ethyl N-ethoxycarbonyliminocarbamate | HCID 220568 | — |
| 反応物 | N-Boc-2-aminophenol | HCID 4935485 | — |
| 反応物 | (1-(Pyridin-4-YL)piperidin-4-YL)methanol | HCID 11310048 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 2-[1-(4-Pyridyl)piperidin-4-ylmethoxy]aniline | HCID 21080292 | 236.4% |
反応手順
To a solution of 1-(4-pyridyl)piperidin-4-ylmethanol (357 mg) and 2-tert-butyloxycarbonylaminophenol (328 mg) in tetrahydrofuran (15 ml) was added triphenylphosphine (447 mg) followed by diethyl azodicarboxylate (0.27 ml). The mixture was stirred at room temperature for 18 hours. The reaction mixture was concentrated to a gum which was purified by column chromatography on silica eluting with methanol/dichloromethane (10:90) to give the tert-butyloxycarbonyl protected derivative of 2-[1-(4-pyridyl)piperidin-4-ylmethoxy]aniline (1.05 g);
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07173025B1 |
| 出典データセット | uspto-grants-2007_02 |
| ORD ID | ord-d422d900877642118b1fc47c2f655ce1 |
| 出典メモ | uspto-grants-2007_02 |