反应详情

温度

85 °C

(5-Bromoimidazo[1,2-a]pyrazin-8-yl)-(4-morpholin-4-ylphenyl)carbamic acid tert-butyl ester (50 mg, 0.11 mmol), 2-fluoro-4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-6-(trifluoromethyl)pyridine (126 mg, 0.21 mmol), KOAc (31 mg, 0.32 mmol) and Pd(dppf)Cl2DCM (4.3 mg, 0.0053 mmol) are stirred under N2 in dioxane (0.3 mL) and heated at 85° C. for 2.5 h. The mixture is cooled and partitioned between NaHCO3 (5% aq., 5 mL) and EtOAc (15 mL). The layers are separated and the aqueous phase extracted with further EtOAc (2×10 mL). The combined organic extracts are washed with brine (10 mL), dried over Na2SO4 and evaporated under reduced pressure to afford the title compound as a brown oil (93 mg) which was used without further purification.

1. temperatureThe mixture is cooled
2. custompartitioned between NaHCO3 (5% aq., 5 mL) and EtOAc (15 mL)
3. customThe layers are separated
4. extractionthe aqueous phase extracted with further EtOAc (2×10 mL)
5. washThe combined organic extracts are washed with brine (10 mL)
6. dry with materialdried over Na2SO4
7. customevaporated under reduced pressure