反应详情

Trifluoroacetic acid (10 mL, 134.63 mmol) was added to a solution of the tert-butyl N-[(3S)-1-methyl-2-oxo-3-[3-[4-[3-(trifluoromethoxy)phenyl]-2-pyridyl]prop-2-ynyl]pyrrolidin-3-yl]carbamate (which may be prepared as described in Description 10) (5.38 g, 10.99 mmol) in DCM (50 mL) at 20° C. and the reaction was stirred until complete. Solid K2CO3 was added to quench the TFA present and the mixture was diluted with water. The phases were separated and the aqueous layer was washed with dichloromethane (×2). The combined organic layers were dried (MgSO4) and the solvent was evaporated to give the (3S)-3-amino-1-methyl-3-[3-[4-[3-(trifluoromethoxy)phenyl]-2-pyridyl]prop-2-ynyl]pyrrolidin-2-one (D11) (4.78 g, 12.276 mmol, 111.7% yield) as an amber oil containing some Ph3PO;

1. customto quench the TFA present
2. additionthe mixture was diluted with water
3. customThe phases were separated
4. washthe aqueous layer was washed with dichloromethane (×2)
5. dry with materialThe combined organic layers were dried (MgSO4)
6. customthe solvent was evaporated