反应详情

[1,5]Naphthyridin-4-ylamine (Intermediate 486) (60 mg, 0.41 mmol) was added to a suspension of NaH (60% in mineral oil; 25 mg, 0.53 mmol) in THF (2 ml) at 0° C. followed by a solution of benzenesulfonyl chloride (95 mg, 0.53 mmol) in THF (1 ml). The mixture was stirred at room temperature for 12 h. After completion, the reaction was quenched with water (5 ml) and the aqueous phase was extracted with EtOAc (30 ml). The organic phase was washed with brine, dried (Na2SO4) and concentrated in vacuo. The crude residue was purified by column chromatography with DCM/MeOH (98:2) as the eluent to give the title compound (30 mg, 30%).

1. customAfter completion, the reaction was quenched with water (5 ml)
2. extractionthe aqueous phase was extracted with EtOAc (30 ml)
3. washThe organic phase was washed with brine
4. dry with materialdried (Na2SO4)
5. concentrationconcentrated in vacuo
6. customThe crude residue was purified by column chromatography with DCM/MeOH (98:2) as the eluent