反应详情

A solution of Example C2 (0.15 g, 0.357 mmol) in DCM (5 mL) was treated portion-wise with mCPBA (0.11 g, 0.43 mmol), stirred at RT overnight, treated with methylamine (2.0M in THF, 3.6 mL, 7.2 mmol) and stirred at RT for 4 h. The mixture was treated with satd. NaHCO3, extracted with DCM (3×) and the combined organics were dried over Na2SO4, concentrated to dryness and purified via silica gel chromatography (MeOH/DCM) to obtain 4-methoxy-N-methyl-5-(6-methyl-5-((2-(1-methyl-1H-pyrazol-4-yl)pyridin-4-yl)oxy)pyridin-2-yl)pyrimidin-2-amine (100 mg, 70%). MS (ESI) m/z: 404.2 (M+H+).

1. stirringstirred at RT for 4 h
2. additionThe mixture was treated with satd
3. extractionNaHCO3, extracted with DCM (3×)
4. dry with materialthe combined organics were dried over Na2SO4
5. concentrationconcentrated to dryness
6. custompurified via silica gel chromatography (MeOH/DCM)