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Ethyl Acetate → 2-[1-(3,4-Dimethoxy-benzyl)-6,7-dimethoxy-1,2,3,4-tetrahydro-naphthalen-2-yl]-N-indan-1-yl-2-phenyl-acetamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Ethyl Acetate | HCID 8857 | — |
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | (+-)-1-Aminoindan | HCID 123445 | — |
| 反応物 | PyBOP | HCID 2724699 | — |
| 反応物 | 1-[(3,4-Dimethoxy-benzyl)-6,7-dimethoxy-1,2,3,4-tetrahydro-naphthalen-2-yl]-phenyl-acetic acid | HCID 69758875 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 2-[1-(3,4-Dimethoxy-benzyl)-6,7-dimethoxy-1,2,3,4-tetrahydro-naphthalen-2-yl]-N-indan-1-yl-2-phenyl-acetamide | HCID 22742835 | 64% |
反応手順
To a solution of 1-[(3,4-Dimethoxy-benzyl)-6,7-dimethoxy-1,2,3,4-tetrahydro-naphthalen-2-yl]-phenyl-acetic acid (100 mg, 0.209 mmol) in 5 ml of dry DMF, were added PyBOP (109 mg, 0.209 mmol), 1-aminoindane (32.3 mg, 0.19 mmol) and dropwise diisopropylethylamine (Hünig's base). (75 μl, 0.437 mmol). The mixture reaction was stirred at RT under argon for 20 h. The mixture was then dissolved in CH2Cl2 and washed with water. The aqueous phase was extracted twice with CH2Cl2, the combined organic extracts were dried over MgSO4, filtered and concentrated to give a crude brown residue. Flash chromatography (AcOEt) gave 72 mg (64%) of the title compound as a pale brown oil.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06703392B2 |
| 出典データセット | uspto-grants-2004_03 |
| ORD ID | ord-527294e8a58b45c3b7dcceae1de8be76 |
| 出典メモ | uspto-grants-2004_03 |