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HRID 244471作成日:2026年10月26日
1-Methyl-3-(trifluoroacetyl)-1H-indole → 2,2,2-Trifluoro-1-[3-(4-fluorophenyl)imidazo[1,5-a]pyridin-7-yl]-1-(1-methyl-1H-indol-3-yl)ethanol
https://huagongshe.com/reaction/244471
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
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| 反応物 | 1-Methyl-3-(trifluoroacetyl)-1H-indole | HCID 3524388 | — |
| 反応物 | 7-Bromo-3-(4-fluorophenyl)imidazo[1,5-a]pyridine | HCID 59437239 | — |
| 反応物 | Butyllithium | HCID 178418339 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 2,2,2-Trifluoro-1-[3-(4-fluorophenyl)imidazo[1,5-a]pyridin-7-yl]-1-(1-methyl-1H-indol-3-yl)ethanol | HCID 24959819 | 34.1% |
反応手順
To a chilled (−78° C.) solution of 7-bromo-3-(4-fluorophenyl)imidazo[1,5-a]pyridine (58 mg, 0.2 mmol) in anhydrous THF (1 mL) was added n-butyllithium (0.1 mL of a 2.5 M solution in hexanes, 2.5 mmol). After 1 minute, a chilled (−78° C.) solution of 2,2,2-trifluoro-1-(1-methyl-1H-indol-3-yl)ethanone (68 mg, 0.3 mmol) in 1 mL of THF was added. After 5 minutes, the reaction mixture was quenched with 50 mL of brine solution and extracted with three 25 mL portions of methylene chloride. The combined organic extracts were washed with water, dried over anhydrous sodium sulfate, and concentrated in vacuo to afford a yellow oil. The residue was purified by column chromatography over silica gel eluting with 0-70% ethyl acetate to afford 30 mg of the title compound as a light yellow solid. MS m/z 440 (MH+).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08658637B2 |
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| 出典データセット | uspto-grants-2014_02 |
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| ORD ID | ord-f76daba1af29439583acd6d6a77d06fb |
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| 出典メモ | uspto-grants-2014_02 |
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