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HRID 1274387作成日:2026年10月26日
Trifluoroacetic acid → 2-[3-(2-Aminoethyl)-2-(3,5-dimethylphenyl)-1H-indol-5-yl]-1-(7-azabicyclo[2.2.1]hept-7-yl)-2-methyl-propan-1-one
https://huagongshe.com/reaction/1274387
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
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| 反応物 | Trifluoroacetic acid | HCID 6422 | — |
| 反応物 | Anisole | HCID 7519 | — |
| 反応物 | {2-[5-[2-(7-azabicyclo[2.2.1]hept-7-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethylphenyl)-1H-indol-3-yl]ethyl}carbamic acid tert-butyl ester | HCID 11114148 | — |
| 生成物 | 2-[3-(2-Aminoethyl)-2-(3,5-dimethylphenyl)-1H-indol-5-yl]-1-(7-azabicyclo[2.2.1]hept-7-yl)-2-methyl-propan-1-one | HCID 11761791 | 95.9% |
反応手順
To a solution of {2-[5-[2-(7-aza-bicyclo[2.2.1]hept-7-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethylphenyl)-1H-indol-3-yl]-ethyl} carbamic acid tert-butyl ester (252 mg in 10 mL methylene chloride) at 0° C. was added 0.60 mL anisole followed by 3.7 mL trifluoroacetic acid and the mixture stirred at 0° C. After 1.5 hours, the mixture was concentrated in vacuo and the residual acid removed by azeotrope with toluene. Purifiaction by flash chromatography on silica gel (methylene chloride:methanol:ammonium hydroxide, 90:7:1) gave the title compound (196 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US06156767 |
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| 出典データセット | uspto-grants-2000_12 |
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| ORD ID | ord-880a0d89374d497f823b7632e329413d |
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| 出典メモ | uspto-grants-2000_12 |
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