反应详情

A solution of 9-borabicyclo[3.3.1]nonane in tetrahydrofuran (0.5M, 1.07 ml, 0.537 mmol) was added to a stirred solution of 1-(6,7-dichloro-2,3-dimethyoxyquinoxalin-5-yl)-3-butenyl methyl sulphone (Example 93 (a)) (200 mg, 0.511 mmol) at room temperature under nitrogen. The mixture was stirred for 20 hours and then trimethylamine N-oxide (119 mg, 1.58 mmol) was added in portions. The mixture was stirred at room temperature for 2 hours and then at reflux for 30 minutes, cooled and concentrated under reduced pressure. The residue was purified by flash chromatography (eluting with 1:1 hexane:ethyl acetate then neat ethyl acetate) to give 1-(6,7-dichloro-2,3-dimethoxyquinoxalin-5-yl)-4-hydroxybutyl methyl sulphone (120 mg, 57%) as a mixture of diastereoisomers (by 1HNMR).

1. stirringThe mixture was stirred at room temperature for 2 hours
2. temperatureat reflux for 30 minutes
3. temperaturecooled
4. concentrationconcentrated under reduced pressure
5. customThe residue was purified by flash chromatography (
6. washeluting with 1:1 hexane