反应详情

A mixture of tert-butyl ((2S)-1-((2-(4-(2-(2,2-difluorocyclopropyl)ethoxy)phenyl)[1,3]oxazolo[4,5-c]pyridin-6-yl)oxy)propan-2-yl)carbamate (239 mg), 4M hydrogen chloride/ethyl acetate (3 mL) and ethyl acetate (3 mL) was stirred at room temperature overnight. The reaction mixture was concentrated under reduced pressure, and the obtained residue was mixed with acetic anhydride (0.138 mL) and pyridine (3 mL), and the obtained mixture was stirred at room temperature for 1 hr. To the reaction mixture was added 1M hydrochloric acid, and the mixture was extracted with ethyl acetate. The combined organic layer were washed with saturated brine, and dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure. The residue was recrystallized (ethyl acetate) to give the title compound (155 mg).

1. concentrationThe reaction mixture was concentrated under reduced pressure
2. additionthe obtained residue was mixed with acetic anhydride (0.138 mL) and pyridine (3 mL)
3. stirringthe obtained mixture was stirred at room temperature for 1 hr
4. additionTo the reaction mixture was added 1M hydrochloric acid
5. extractionthe mixture was extracted with ethyl acetate
6. washThe combined organic layer were washed with saturated brine
7. dry with materialdried over anhydrous magnesium sulfate
8. customthe solvent was evaporated under reduced pressure
9. customThe residue was recrystallized (ethyl acetate)