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Water → 3-Chloro-N-[1-(2-chlorophenyl)-2-[1-(2,2,2-trifluoroethyl)-piperidin-4-ylmethoxy]ethyl]-1H-indole-6-carboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 2,2,2-Trifluoroethyl trifluoromethanesulfonate | HCID 80366 | — |
| 反応物 | 3-chloro-N-[1-(2-chlorophenyl)-2-(piperidin-4-ylmethoxy)ethyl]-1H-indole-6-carboxamide | HCID 69307888 | — |
| 溶媒 | Dimethyl Sulfoxide | HCID 679 | — |
| 生成物 | 3-Chloro-N-[1-(2-chlorophenyl)-2-[1-(2,2,2-trifluoroethyl)-piperidin-4-ylmethoxy]ethyl]-1H-indole-6-carboxamide | HCID 69309741 | 30% |
反応手順
To a solution of 3-chloro-N-[1-(2-chlorophenyl)-2-(piperidin-4-ylmethoxy)ethyl]-1H-indole-6-carboxamide (700 mg, 1.6 mmol) in 5 mL of DMSO was added potassium carbonate (1.0 g, 7.9 mmol) and 2,2,2-trifluoroethyl trifluoromethane-sulfonate (364 mg, 1.6 mmol). The reaction was allowed to stir at room temperature overnight after which time water was added and the resulting precipitate was isolated by filtration. Purification of the filtrate (SiO2: 30% EtOAc in hexane) provided 250 mg (30%) of the title compound.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07427632B2 |
| 出典データセット | uspto-grants-2008_09 |
| ORD ID | ord-7363ab9554e2406d92b955252c986d5c |
| 出典メモ | uspto-grants-2008_09 |