反应详情

温度

140 °C

A mixture of (2-bromo-3-methylphenyl)(pyrimidin-4-yl)methanone (0.10 g, 0.361 mmol), 3-morpholino-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)quinolin-2-amine (0.192 g, 0.541 mmol, prepared as in Example 2, Step 1-2), potassium phosphate tribasic (0.149 mL, 1.804 mmol), Pd2dba3 (0.033 g, 0.036 mmol), and 2-(dicyclohexylphosphino)-2′,4′,6′,-tri-1-propyl-1,1′-biphenyl (0.034 g, 0.072 mmol) in dioxane/water (3/1.5 mL) was heated in mw for 12 min at 140° C. The mixture was concentrated and the resulting crude material was chromatographed on silica gel using 0-5% 2M NH3 in MeOH/DCM to afford a brown oil which was further purified by HPLC to afford (2-(2-amino-3-morpholinoquinolin-6-yl)-3-methylphenyl)(pyrimidin-4-yl)methanone as a yellow solid. MS (ESI, pos. ion) m/z: 426 (M+1).

1. concentrationThe mixture was concentrated
2. customthe resulting crude material was chromatographed on silica gel using 0-5% 2M NH3 in MeOH/DCM
3. customto afford a brown oil which
4. customwas further purified by HPLC