(E)-Methyl 3-(2-amino-4-fluorophenyl)acrylate → 7-Fluoroquinolin-2(1H)-one
反応式
[NH2:1][C:2]1[CH:7]=[C:6]([F:8])[CH:5]=[CH:4][C:3]=1/[CH:9]=[CH:10]/[C:11]([O:13]C)=O>C1COCC1.Cl>[F:8][C:6]1[CH:7]=[C:2]2[C:3]([CH:9]=[CH:10][C:11](=[O:13])[NH:1]2)=[CH:4][CH:5]=1参加物
4
反応条件
- 温度
- 65 °C
実験手順
A mixture of (E)-methyl 3-(2-amino-4-fluorophenyl)acrylate (30.38 g, 156 mmol) in THF (400 mL) and 3M hydrochloric acid (400 mL) was heated at 65° C. for 20 h. The mixture was cooled to RT and poured onto ice. The resulting precipitate was filtered, washed with copious amounts of water and dried in vacuo to give 20.65 g (81%) of a light-yellow amorphous solid. m/z=164 (M+1).
後処理
- temperatureThe mixture was cooled to RT
- additionpoured onto ice
- filtrationThe resulting precipitate was filtered
- washwashed with copious amounts of water
- customdried in vacuo
出典と根拠
- ORDレコード
- ord-9ba7fd3c05aa4d91a64c2e198ff35b4b
- 出典データセット
- uspto-grants-2016_04
- 特許番号
- US09303028B2
反応ノート
読み込み中…