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[1-(3-Ethoxy-4-methoxy-benzyl)-piperidin-4-yl]-carbamic acid tert-butyl ester → 1-(3-Ethoxy-4-methoxy-benzyl)-piperidin-4-ylamine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | [1-(3-Ethoxy-4-methoxy-benzyl)-piperidin-4-yl]-carbamic acid tert-butyl ester | HCID 67147361 | — |
| 溶媒 | Hydrochloric Acid | HCID 313 | — |
| 溶媒 | Ethanol | HCID 702 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | 1-(3-Ethoxy-4-methoxy-benzyl)-piperidin-4-ylamine | HCID 39257445 | 89% |
反応手順
A solution of [1-(3-ethoxy-4-methoxy-benzyl)-piperidin-4-yl]-carbamic acid tert-butyl ester (9.71 g, 26.64 mmol) in ethanol (50 mL) and 4 M HCl in dioxane (75 mL) was stirred at rt for 2 h. The hydrochloric acid was removed under reduced pressure and the crude reaction product extracted from a solution of 1 M NaOH (200 mL) with ethyl acetate (3×100 mL). The combined organic phases were dried over MgSO4 and concentrated by evaporation under reduced pressure yielding 4.69 g (89%) of the title compound as a white solid. The crude material was directly used in the following reaction step without further purification. MS (ISP): 265.0 [M+H]+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07855194B2 |
| 出典データセット | uspto-grants-2010_12 |
| ORD ID | ord-084a776b4cdc49a1aed2c86f035799f7 |
| 出典メモ | uspto-grants-2010_12 |