反应详情

To a stirred solution of 3-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-5-(6-formylpyridin-3-yl)-N-((4-isopropyl-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methylbenzamide (0.28 g, 0.528 mmol) and morpholine (0.07 g, 0.79 mmol) in dichloroethane (3 mL), acetic acid (0.19 g, 3.16 mmol) was added and reaction stirred at room temperature for 20 minutes. Then sodium triacetoxyborohydride (0.33 g, 1.55 mmol) was added at 0° C. and reaction stirred at room temperature for 2 h. On completion, reaction was quenched with aqueous sodium bicarbonate, organic phase was separated and aqueous phase was extracted with dichloromethane. Combined organic layers were dried over sodium sulphate and concentrated under reduced pressure to give crude material was purified by prep. HPLC to afford the title compound (0.12 g, 38.70%).

1. customreaction
2. customreaction
3. stirringstirred at room temperature for 2 h
4. customOn completion, reaction
5. customwas quenched with aqueous sodium bicarbonate, organic phase
6. customwas separated
7. extractionaqueous phase was extracted with dichloromethane
8. dry with materialCombined organic layers were dried over sodium sulphate
9. concentrationconcentrated under reduced pressure
10. customto give crude material
11. customwas purified by prep