反应详情

Hydrogen chloride in dioxane 4M (15 mL, 60.1 mmol) was added to 8-(1-((R)-1,1-dimethylethylsulfinamido)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (2.7 g, 6.0 mmol) dissolved in dioxane (40 mL). The resulting white suspension was stirred at RT for 1 hour, collected by filtration, washed with diethyl ether and dried. It was dissolved into a 5% methanolic ammonia (7 N) sol. in DCM (200 mL) and stirred for 5 minutes. The precipitate (NH4Cl) was removed by filtration and the filtrate was concentrated to dryness to afford 8-(1-aminoethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (single enantiomer, 1.85 g, 89%) as an off-white solid. Mass Spectrum: M+H+ 346. [α]D20°: +35° in acetonitrile.

1. filtrationcollected by filtration
2. washwashed with diethyl ether
3. customdried
4. dissolutionIt was dissolved into a 5% methanolic ammonia (7 N) sol. in DCM (200 mL)
5. stirringstirred for 5 minutes
6. customThe precipitate (NH4Cl) was removed by filtration
7. concentrationthe filtrate was concentrated to dryness