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Water → 3-Chloro-N-[1-(2-chlorophenyl)-2-[1-(2,2,2-trifluoroacetyl)-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 | Triethylamine | HCID 8471 | — |
| 反応物 | Ethyl trifluoroacetate | HCID 9794 | — |
| 反応物 | 3-chloro-N-[1-(2-chlorophenyl)-2-(piperidin-4-ylmethoxy)ethyl]-1H-indole-6-carboxamide | HCID 69307888 | — |
| 溶媒 | Methanol | HCID 887 | — |
| 生成物 | 3-Chloro-N-[1-(2-chlorophenyl)-2-[1-(2,2,2-trifluoroacetyl)-piperidin-4-ylmethoxy]ethyl]-1H-indole-6-carboxamide | HCID 86603601 | 42.1% |
反応手順
To a solution of 3-chloro-N-[1-(2-chlorophenyl)-2-(piperidin-4-ylmethoxy)ethyl]-1H-indole-6-carboxamide (600 mg, 1.3 mmol) in 5 mL of methanol was added triethylamine (0.37 mL, 2.7 mmol) and trifluoroacetic acid ethyl ester (0.20 mL, 2.7 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: 10:2:0.5 DCM:hexane:isopropylamine) provided 297 mg (41%) 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-5e244fec7d16455e9dde4969716cd94a |
| 出典メモ | uspto-grants-2008_09 |