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Trifluoroacetic acid → 3-[1-Cyclopropyl-1-(4-methylphenyl)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 | alpha-Cyclopropyl-alpha,4-dimethylbenzenemethanol | HCID 98258 | — |
| 反応物 | 7-[(Methylsulfanyl)methyl]-1H-indole | HCID 58392187 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 3-[1-Cyclopropyl-1-(4-methylphenyl)ethyl]-7-[(methylsulfanyl)methyl]-1H-indole | HCID 58392280 | — |
反応手順
0.23 ml (3.00 mmol) of trifluoroacetic acid was added to 885 mg (4.99 mmol) of the compound from Example 8A and 440 mg (2.50 mmol) of the compound from Example 137A in 44 ml of dichloromethane, and the mixture was stirred at RT overnight. The reaction mixture was concentrated in a rotary evaporator. The residue was purified by preparative HPLC (RP18 column; mobile phase: acetonitrile/water gradient with addition of 0.1% formic acid) to result in 87.4 mg (10% of theory) of the title compound as mixture of diastereomers.
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-4da1d5476b2e4fe384010306eb100e3c |
| 出典メモ | uspto-grants-2011_11 |