反应详情

To a warm solution of 4-(2-{[4-(2-cyclopropyl-1,3-oxazol-4-yl)benzyl]amino}ethyl)phenol (0.42 g, 1.25 mmol) in acetonitrile (6 ml) was added Cs2CO3 (1.34 g, 4.11 mmol) followed by ethyl-2-bromoisobutyrate (0.60 mL, 4.09 mmol). The mixture was heated at 80C for 20 h. Upon cooling, the mixture was partitioned between EtOAc and water. The aqueous phase was extracted with EtOAc (2×25 ml). The combined organic phases were dried with MgSO4 and concentrated in vacuo. The crude material was purified by flash chromatography (MeOH/EtOAc, 2:98) to yield ethyl 2-[4-(2-{[4-(2-cyclopropyl-1,3-oxazol-4-yl)benzyl]amino}ethyl)phenoxy]-2-methylpropanoate (0.42 g, 74%).

1. temperatureUpon cooling
2. customthe mixture was partitioned between EtOAc and water
3. extractionThe aqueous phase was extracted with EtOAc (2×25 ml)
4. dry with materialThe combined organic phases were dried with MgSO4
5. concentrationconcentrated in vacuo
6. customThe crude material was purified by flash chromatography (MeOH/EtOAc, 2:98)