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Water → N-{1-(Morpholin-4-ylcarbonyl)-5-[4-(trifluoromethyl)phenyl]piperidin-3-yl}benzenecarboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | 4-Morpholinecarbonyl chloride | HCID 84810 | — |
| 反応物 | N-{5-[4-(trifluoromethyl)phenyl]piperidin-3-yl}benzamide | HCID 66701397 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | N-{1-(Morpholin-4-ylcarbonyl)-5-[4-(trifluoromethyl)phenyl]piperidin-3-yl}benzenecarboxamide | HCID 66701371 | — |
反応手順
At 0° C., 705 mg (2.02 mmol) of N-{5-[4-(trifluoromethyl)phenyl]piperidin-3-yl}benzamide were initially charged in 70 ml of dichloromethane, and 321 mg (2.02 mmol) of morpholine-4-carbonyl chloride and 564 μl (4.04 mmol) of triethylamine were added. The mixture was slowly warmed to RT overnight. Water was added, and the reaction mixture was extracted. The organic phase was dried over magnesium sulphate and concentrated under reduced pressure. The residue was then purified by preparative HPLC (Reprosil C18, water/acetonitrile gradient). Yield: 960 mg (100% of theory)
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08987248B2 |
| 出典データセット | uspto-grants-2015_03 |
| ORD ID | ord-358e3ad6b1374a59afa264e74a909f13 |
| 出典メモ | uspto-grants-2015_03 |