反应详情

5-Bromo-6-(4-chlorophenyl)-2-pyrazinecarboxylic acid methyl ester (CAN 960247-79-4, 2.420 g, 7.39 mmol) was dissolved in dry DMSO (25 mL). Cesium carbonate (4.41 g, 8.13 mmol) and (S)-1,1,1-trifluoropropan-2-ol (927 mg, 8.13 mmol) were added and the reaction mixture was stirred at room temperature for 2 h. The mixture was partitioned between water and ethyl acetate; the organic phase was dried with MgSO4 and concentrated in vacuo. The crude residue was purified by flash chromatography (silica gel, 100 g, 10% to 50% ethyl acetate in heptane) to yield 2.53 g (95%) of the title compound as yellow oil; MS (EI) 361.1 (M+H)+.

1. customThe mixture was partitioned between water and ethyl acetate
2. dry with materialthe organic phase was dried with MgSO4
3. concentrationconcentrated in vacuo
4. customThe crude residue was purified by flash chromatography (silica gel, 100 g, 10% to 50% ethyl acetate in heptane)