反应详情

温度

100 °C

In a microwave vial containing 5-bromo-6-{4-[1-(2-dimethylamino-ethyl)-4-(4-fluoro-3-trifluoromethyl-phenyl)-1H-imidazol-2-yl]-piperidin-1-yl}-pyrimidin-4-ylamine (70.00 mg; 0.13 mmol; 1.00 eq.) in Toluene (3.50 ml) and water (0.35 ml) was added 2-cyclopropyl-4,4,5,5-tetramethyl-[1,3,2]dioxaborolane (0.09 ml; 0.50 mmol; 4.00 eq.), Palladium acetate (4.24 mg; 0.02 mmol; 0.15 eq.), Tricyclohexyl-phosphane (10.58 mg; 0.04 mmol; 0.30 eq.) and Potassium phosphonate (112.16 mg; 0.53 mmol; 4.20 eq.). The mixture was stirred at 100° C. for 5 h before the reaction mixture was filtered, concentrated and purified via waters pre-HPLC. LC-MS: (M+1=518, obsd.=518).

1. filtrationwas filtered
2. concentrationconcentrated
3. custompurified via waters pre-HPLC