反应详情

To a solution of tert-butyl 6-(morpholinomethyl)pyridin-3-ylcarbamate (115; 1.20 g, 4.1 mmol) in dichloromethane (20 mL) was added TFA (6.0 mL). The resulting reaction mixture was stirred at room temperature for 12 h and then concentrated under reduced pressure. Enough saturated aqueous Na2CO3 was added to the residue to adjust the pH=9. The mixture was extracted with ethyl acetate (3×25 mL). The combined organic layers were dried (Na2SO4) and concentrated under reduced pressure to afford 6-(morpholinomethyl)pyridin-3-amine 116 (450 mg, 56%).

1. customThe resulting reaction mixture
2. concentrationconcentrated under reduced pressure
3. additionEnough saturated aqueous Na2CO3 was added to the residue
4. extractionThe mixture was extracted with ethyl acetate (3×25 mL)
5. dry with materialThe combined organic layers were dried (Na2SO4)
6. concentrationconcentrated under reduced pressure