反应详情

To a solution of 3-(aminomethyl)-4-(ethylsulfonyl)aniline (1.1 g, 5.1 mmol) in DMF (5 mL) and TEA (2.75 mL) was added benzyl 2,5-dioxopyrrolidin-1-yl carbonate (1.4 g, 5.7 mmol) in DCM (15 mL). The solution was stirred for 18 h before quenching with water (25 mL). The reaction mixture was extracted with DCM (2×30 mL), washed with brine and dried (MgSO4). The organic layer was concentrated in vacuo and the residue purified by flash chromatography (0-100% EtOAc/Hexane) to afford 28A (1.0 g, 59%) as an oil. MS (ESI) m/z 349.2 (M+H)+.

1. custombefore quenching with water (25 mL)
2. extractionThe reaction mixture was extracted with DCM (2×30 mL)
3. washwashed with brine
4. dry with materialdried (MgSO4)
5. concentrationThe organic layer was concentrated in vacuo
6. customthe residue purified by flash chromatography (0-100% EtOAc/Hexane)