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Tropic acid → 3-Hydroxy-2-phenyl-1-pyrrolidin-1-yl propan-1-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Tropic acid | HCID 10726 | — |
| 反応物 | Pyrrolidine | HCID 31268 | — |
| 反応物 | HOAt | HCID 181649 | — |
| 反応物 | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 3-Hydroxy-2-phenyl-1-pyrrolidin-1-yl propan-1-one | HCID 68706980 | — |
反応手順
To a solution of tropic acid (0.12 mmol) and pyrrolidine (0.12 mmol) in DMF (20 mL) are added HOAt (0.18 mmol) and EDCI-HCl (0.18 mmol). The reaction mixture is stirred at room temperature for 14 h. The reaction mixture is diluted with water, then extracted with AcOEt. The organic extracts are successively washed with water, sat. aq, NaHCO3, H2O and brine, dried over Na2SO4, filtered, and concentrated in vacuo. The residue is purified by silica gel column chromatography to give 3-hydroxy-2-phenyl-1-pyrrolidin-1-yl propan-1-one.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07704996B2 |
| 出典データセット | uspto-grants-2010_04 |
| ORD ID | ord-15157d95db1648df88d50d6902912257 |
| 出典メモ | uspto-grants-2010_04 |