反应详情

To a solution of tert-butyl 6-(pyrrolidin-1-ylmethyl)pyridin-2-ylcarbamate (96; 750 mg, 2.7 mmol) in dichloromethane (10 mL) was added TFA (4.0 mL) at room temperature. The resulting reaction mixture was stirred at room temperature for 6 h and then concentrated under reduced pressure. Enough saturated aqueous Na2CO3 was added to the resulting residue to adjust the pH=9. The mixture was then extracted with ethyl acetate (3×25 mL). The combined organic layers were dried (Na2SO4) and concentrated under reduced pressure to afford 6-(pyrrolidin-1-ylmethyl)pyridin-2-amine 97 (440 mg, 92%).

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