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Trifluoroacetic acid → (3R,6S)-3-Amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Trifluoroacetic acid | HCID 6422 | — |
| 反応物 | 1,1-Dimethylethyl N-((3R,6S)-6-(2,3-difluorophenyl)hexahydro-2-oxo-1-(2,2,2-trifluoroethyl)-1H-azepin-3-yl)carbamate | HCID 86595042 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | (3R,6S)-3-Amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one | HCID 23653826 | — |
反応手順
To a solution of tert-butyl (3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-ylcarbamate from Step F (135 mg, 0.320 mmol) in CH2Cl2 (5 mL) was added CF3CO2H (2.5 mL). After 30 min, the solution was concentrated in vacuo and azeotroped with toluene (2×). Saturated aqueous NaHCO3 was added and the mixture was extracted with CH2Cl2 (3×). The combined organic extracts were washed with brine, dried over MgSO4, filtered and concentrated in vacuo to give the title compound. MS: m/z=323 (M+1).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07390798B2 |
| 出典データセット | uspto-grants-2008_06 |
| ORD ID | ord-0c228504b75043de85c9f06cdf76478a |
| 出典メモ | uspto-grants-2008_06 |