反应详情

温度

80 °C

To a solution of (S)-3-(3-bromopyrazolo[1,5-a]pyrimidin-5-yl)-4-phenyloxazolidin-2-one (0.20 g, 0.56 mmol), 3-(2-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-1,2,4-triazole (0.35 g, 0.84 mmol) and sodium carbonate (2.0 M, 1.4 ml, 2.8 mmol) in dioxanes (30 mL) was degassed with nitrogen for 30 minutes. Pd2 dba3 (70 mg) and XPHOS (70 mg) were added and the reaction was heated to 80° C. for 4 hours. The reaction was poured into EtOAc and the layers separated. The organic layer was washed with water, brine, dried over MgSO4 and concentrated in vacuo. The crude material was purified by normal phase chromatography, using 25% EtOAc/DCM as the eluent to give (S)-3-(3-(3-fluoro-4-(1-((2-(trimethylsilyl)ethoxy)methyl)-1H-1,2,4-triazol-3-yl)phenyl)pyrazolo[1,5-a]pyrimidin-5-yl)-4-phenyloxazolidin-2-one as a solid (0.30 g, 0.52 mmol, 94% yield).

1. customthe layers separated
2. washThe organic layer was washed with water, brine
3. dry with materialdried over MgSO4
4. concentrationconcentrated in vacuo
5. customThe crude material was purified by normal phase chromatography