反应详情

温度

100 °C

Pd(OAc)2 (0.233 g, 1 mmol) was added to a degassed mixture of 2-(4-fluorophenyl)-8-isopropoxyimidazo[1,2-a]pyrazine (1.43 g, 5.2 mmol), 4-iodo-2-(methylthio)pyrimidine (Frontier, 1.96 g, 7.8 mmol), Cs2CO3 (2.57 g, 7.8 mmol) and PPh3 (0.54 g, 2 mmol) in DMF (6 mL). The resulting reaction mixture was heated at about 100° C. for about 4 h, cooled to ambient temperature, and partitioned between EtOAc and brine. The organic layer was separated, dried over MgSO4, filtered, and evaporated. The crude material was purified by silica gel chromatography using heptane/EtOAc (gradient, 100%/0% to 50%/50%) to afford 1.05 g (51%) of the title compound: LC/MS (Table 1, Method g) Rt=3.45 min; MS m/z: 396.2 (M+H)+.

1. customThe resulting reaction mixture
2. temperaturecooled to ambient temperature
3. custompartitioned between EtOAc and brine
4. customThe organic layer was separated
5. dry with materialdried over MgSO4
6. filtrationfiltered
7. customevaporated
8. customThe crude material was purified by silica gel chromatography