反应详情

To a solution of 1-[2-(4-amino-1-piperidinyl)ethyl]-7-fluoro-2(1H)-quinoxalinone dihydrochloride (0.363 g, 1 mmol) in dry MeOH (5 ml) was added a 25 wt. % solution of sodium methoxide in MeOH (0.87 ml, 4 mmol). After heating under reflux overnight, a further portion of sodium methoxide solution (0.22 ml) was added and heating was continued for 24 h. Aqueous ammonium chloride 96 drops) was added and the mixture was evaporated to dryness. The residue was extracted several times with 10% MeOH/DCM, and the extracts were filtered and evaporated. The residue was chromatographed on silica, eluting with 0-20% (2M ammonia/MeOH)/DCM to give the product (0.20 g, 66%).

1. temperatureAfter heating
2. temperatureunder reflux overnight
3. temperatureheating
4. customthe mixture was evaporated to dryness
5. extractionThe residue was extracted several times with 10% MeOH/DCM
6. filtrationthe extracts were filtered
7. customevaporated
8. customThe residue was chromatographed on silica
9. washeluting with 0-20% (2M ammonia/MeOH)/DCM