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Trifluoroacetic acid → 3-[1-Cyclopropyl-1-(4-fluorophenyl)ethyl]-7-[(methylsulfanyl)methyl]-1H-indole
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Trifluoroacetic acid | HCID 6422 | — |
| 反応物 | 1-Cyclopropyl-1-(4-fluorophenyl)ethanol | HCID 98104 | — |
| 反応物 | 7-[(Methylsulfanyl)methyl]-1H-indole | HCID 58392187 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 3-[1-Cyclopropyl-1-(4-fluorophenyl)ethyl]-7-[(methylsulfanyl)methyl]-1H-indole | HCID 58392106 | — |
反応手順
559 mg (3.10 mmol) of the compound from Example 77A and 0.26 ml (3.39 mmol) of trifluoroacetic acid were added to 500 mg (2.82 mmol) of the compound from Example 8A in 12 ml of dichloromethane. The reaction mixture was stirred at RT for 30 min and then diluted with dichloromethane, washed with saturated aqueous sodium bicarbonate solution and saturated aqueous sodium chloride solution, dried over sodium sulfate, filtered and concentrated. Purification of the crude product by preparative HPLC (mobile phase: acetonitrile/water gradient) resulted in 361 mg (38% of theory) of the title compound.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08063234B2 |
| 出典データセット | uspto-grants-2011_11 |
| ORD ID | ord-0be2306708914b3e9eb50432c2e77ae8 |
| 出典メモ | uspto-grants-2011_11 |