Water → 6-Fluoro-7-hydroxy-3,4-dihydroisoquinolin-1(2H)-one
反応式
[F:1][C:2]1[CH:3]=[C:4]2[C:9](=[CH:10][C:11]=1[O:12]C)[C:8](=[O:14])[NH:7][CH2:6][CH2:5]2.B(Br)(Br)Br.O.CCOC(C)=O>C(Cl)Cl>[F:1][C:2]1[CH:3]=[C:4]2[C:9](=[CH:10][C:11]=1[OH:12])[C:8](=[O:14])[NH:7][CH2:6][CH2:5]2参加物
6
実験手順
To a 0° C. solution of 6-fluoro-7-methoxy-3,4-dihydroisoquinolin-1(2H)-one (Cpd M, 0.428 g, 2.19 mmol) in DCM (15 mL) was added boron tribromide (1.0M in DCM, 6.00 mL, 6.00 mmol). The reaction mixture was stirred for 1 hour, then the reaction mixture was allowed to warm to room temperature. After stirring for 4 hours, water (25 mL) and EtOAc (100 mL) were added and the mixture was stirred vigorously. The layers were separated, and the organic layer was filtered and concentrated under vacuum to give 6-fluoro-7-hydroxy-3,4-dihydroisoquinolin-1(2H)-one (Cpd N, 355 mg, 89%).
後処理
- stirringAfter stirring for 4 hours
- stirringthe mixture was stirred vigorously
- customThe layers were separated
- filtrationthe organic layer was filtered
- concentrationconcentrated under vacuum
出典と根拠
- ORDレコード
- ord-795a15b2a98f47dbae2a664056b1beb2
- 出典データセット
- uspto-grants-2015_05
- 特許番号
- US09040515B2
反応ノート
読み込み中…