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Phenylhydrazine → 2-(4-Fluorophenyl)-3-(4-(methylsulfonyl)phenyl)indole
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Phenylhydrazine | HCID 7516 | — |
| 反応物 | 1-(4-Fluorophenyl)-2-(4-methylsulfonylphenyl)ethanone | HCID 11243301 | — |
| 触媒 | Methanesulfonic Acid | HCID 6395 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 溶媒 | Acetic acid toluene | HCID 18331056 | — |
| 生成物 | 2-(4-Fluorophenyl)-3-(4-(methylsulfonyl)phenyl)indole | HCID 15337397 | 53.6% |
反応手順
A solution of phenylhydrazine (203 uL, 1.73 mmol) and 1-(4-fluorophenyl)-2-(4-(methylsulfonyl)phenyl)ethanone (510 mg, 1.73 mmol) (Step 2) in a mixture of toluene/HOAc (2:1; 5 mL) containing 1 drop of methanesulfonic acid was stirred at r.t. overnight. The reaction mixture was diluted with EtOAc and was washed successively with H2O, 1M NaOH, H2O and dried. Evaporation of the solvent gave a residue which was purified by silica gel chromatography using EtOAc/hexane (1:3+10% CH2Cl2) as eluent to afford 339 mg of the title compound.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06329421B1 |
| 出典データセット | uspto-grants-2001_12 |
| ORD ID | ord-db2bd42e56254025ae9f901673442162 |
| 出典メモ | uspto-grants-2001_12 |