反应详情

To a mixture of crude (2-morpholin-4-yl-ethyl)-[3-{6-[(thiophen-3-ylmethyl)-amino]-pyridin-2-yl}-1-(2-trimethylsilanyl-ethoxymethyl)-1H-pyrazolo[3,4-d]pyrimidin-6-yl]-amine (149 mg, crude) in dichloromethane (2 mL) was added CF3COOH (2 mL). This mixture was stirred at room temperature for 2 hours. The solvent was removed under reduced pressure. A saturated aqueous solution of NaHCO3 was added to the residue, and then extracted with ethyl acetate (3×15 mL). The combined organic phase was dried over anhydrous MgSO4, filtered and concentrated under reduced pressure. The residue was washed with dichloromethane (2 mL) to give (2-morpholin-4-yl-ethyl)-(3-{6-[(thiophen-3-ylmethyl)-amino]-pyridin-2-yl}-1H-pyrazolo[3,4-d]pyrimidin-6-yl)-amine as a white solid. (Yield 46 mg, 18% over two steps).

1. customThe solvent was removed under reduced pressure
2. additionA saturated aqueous solution of NaHCO3 was added to the residue
3. extractionextracted with ethyl acetate (3×15 mL)
4. dry with materialThe combined organic phase was dried over anhydrous MgSO4
5. filtrationfiltered
6. concentrationconcentrated under reduced pressure
7. washThe residue was washed with dichloromethane (2 mL)