化工社化工社 化学情報印刷レポート · 研究参考用
Triethylamine → 4-(3-Morpholinon-4-yl)piperidin-1-yl-2-(2-fluorophenyl)-2-(4-chlorophenylaminocarbonylamino)-acetamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | Benzotriazol-1-yloxy-tris(dimethylamino)phosphonium hexafluorophosphate | HCID 151348 | — |
| 反応物 | Piperidine, hydrochloride (1:1) | HCID 2723721 | — |
| 反応物 | 4-(Piperidin-4-yl)morpholin-3-one hydrochloride | HCID 53255665 | — |
| 反応物 | 2-(2-Fluorophenyl)-2-(4-chlorophenylaminocarbonylamino)-acetic acid | HCID 68695741 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 4-(3-Morpholinon-4-yl)piperidin-1-yl-2-(2-fluorophenyl)-2-(4-chlorophenylaminocarbonylamino)-acetamide | HCID 68690703 | 26.5% |
反応手順
To a solution of 2-(2-fluorophenyl)-2-(4-chlorophenylaminocarbonylamino)-acetic acid (50 mg, 0.15 mmol), 4-(3-morpholinon-4-yl)piperidine hydrochloride (45 mg, 0.20 mmol) and triethylamine (0.086 mL, 0.62 mmol) in DMF (1.0 mL, containing 0.10 mL of H2O to solubilize the piperidine hydrochloride), BOP (100 mg, 0.23 mmol) was added. After being stirred at room temperature for 30 min, the mixture was purified by HPLC to give the titled compound (20 mg). MS 489.4 and 491.4 (M+H, Cl pattern).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07678913B2 |
| 出典データセット | uspto-grants-2010_03 |
| ORD ID | ord-b25e3a9f6369479daab1c94275a37dac |
| 出典メモ | uspto-grants-2010_03 |