反应详情

温度

80 °C

(S)-4-(5-bromopyrimidin-2-yl)-2-((6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)methyl)morpholine (50 mg, 0.11 mmol), 1-(4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolane-2-yl)benzyl)piperazin-1-yl)ethanone (45 mg, 0.13 mmol), Pd(dppf)2Cl2 (4.5 mg, 0.005 mmol), and K2CO3 (45 mg, 0.33 mmol) were dissolved in dioxane (4 ml)+H2O (1 ml), and then degassed with N2 (gas), followed by stirring at 80° C. for 2 hours. After the completion of the reaction, the reaction mixture was extracted with H2O, EA, and brine, followed by drying (Na2SO4), filtration, and concentration under reduced pressure, and the residue was purified by column chromatography (MeOH:MC=1:10), to give (S)-1-(4-(4-(2-(2-((6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine-1-yl)methyl)morpholino)pyrimidin-5-yl)benzyl)piperazin-1-yl)ethanone (58 mg, 90%).

1. customdegassed with N2 (gas)
2. customAfter the completion of the reaction
3. extractionthe reaction mixture was extracted with H2O, EA, and brine
4. customby drying
5. filtration(Na2SO4), filtration, and concentration under reduced pressure
6. customthe residue was purified by column chromatography (MeOH:MC=1:10)