反应详情

温度

80 °C

A solution of Example C4 in dioxane (3 mL) was treated with acetamide (0.06 g, 1.0 mmol), Cs2CO3 (0.11 g, 0.34 mmol), X-Phos (0.03 g, 0.077 mmol) and Pd2(dba)3 (0.03 g, 0.034 mmol) and heated at 80° C. overnight. The mixture was diluted with EtOAc, the solids removed via filtration through diatomaceous earth, washed with EtOAc and the filtrate was washed with water, then brine, dried over Na2SO4, concentrated to dryness and purified by silica gel chromatography (MeOH/DCM) to afford N-(4-((6-(2-(isopropylamino)-4-methoxypyrimidin-5-yl)-2-methylpyridin-3-yl)oxy)pyridin-2-yl)acetamide (60 mg, 36%).

1. customthe solids removed via filtration through diatomaceous earth
2. washwashed with EtOAc
3. washthe filtrate was washed with water
4. dry with materialbrine, dried over Na2SO4
5. concentrationconcentrated to dryness
6. custompurified by silica gel chromatography (MeOH/DCM)