Hydrogen Bromide → Isoindolin-5-ol HCl
反応式
C[O:2][C:3]1[CH:4]=[C:5]2[C:9](=[CH:10][CH:11]=1)[CH2:8][NH:7][CH2:6]2.[BrH:12]>>[BrH:12].[OH:2][C:3]1[CH:4]=[C:5]2[C:9](=[CH:10][CH:11]=1)[CH2:8][NH:7][CH2:6]2参加物
3
実験手順
5-Methoxy-2,3-dihydro-1H-isoindole (28.7 g) was dissolved in 48% hydrobromic acid (620 ml) and the mixture heated under reflux for 2 h, then cooled and evaporated to give 5-hydroxy-2,3-dihydro-1H-isoindole hydrobromide (29.5 g) as a brown solid. To the above hydrobromide salt (29.5 g) in tetrahydrofuran (215 ml) and water (215 ml) at 0° C. was added triethylamine (48 ml) followed by di-tert-butyl dicarbonate (33 g). The reaction was stirred for 18 h, then worked up as for Description 1 above and chromatographed on silica gel, to give the title compound (13.2 g, 29%) as a brown solid.
後処理
- temperaturethe mixture heated
- temperatureunder reflux for 2 h
- temperaturecooled
- customevaporated
出典と根拠
- ORDレコード
- ord-a11314d5656c461ca690a290772da00a
- 出典データセット
- uspto-grants-2003_02
- 特許番号
- US06521638B1
反応ノート
読み込み中…