反应详情

6-[5-(Azetidin-3-yl)-1,2,4-oxadiazol-3-yl]-2-N-methyl-2-N-phenyl-1,3,5-triazine-2,4-diamine (Intermediate 149, 85 mg, 0.26 mmol), 3,3,3-trifluoropropanal (32 μL, 0.28 mmol) and acetic acid (45 μL, 0.78 mmol) were combined in DCE (5 mL) and stirred for 3 h at room temperature. Sodium triacetoxyborohydride (83 mg, 0.39 mmol) was added and the mixture was heated to 70 C for 5 h. The reaction mixture was cooled at room temperature, concentrated under vacuum and purified by preparative HPLC, Method C, to afford the title compound as a white solid (25 mg, 26%).

1. temperaturethe mixture was heated to 70 C for 5 h
2. temperatureThe reaction mixture was cooled at room temperature
3. concentrationconcentrated under vacuum
4. custompurified by preparative HPLC, Method C