反应详情

温度

90 °C

Under Ar, compound, methyl 2-(4-(7-(bis((2-(trimethylsilyl)ethoxy)methyl)amino)-3-iodopyrazolo[1,5-a]pyrimidin-5-yloxy)phenyl)acetate (180 mg, 0.26 mmol) was mixed with Pd(dppf) Cl2 (21 mg, 0.26 mmol, K3PO4 (106 mg, 0.5 mmol), 3-quinoline bornic acid (55 mg, 0.31 mmol) and dioxane (10 mL with 1 ml water). The resulting mixture was heated at 90° C. and stirred over night. After cooled to room temperature, the mixture was diluted with EtOAc (60 mL) and filtered through celite. After concentration, the crude was purified with column (silica gel, 0˜30% EtOAc/Hexane) gave the product, methyl 2-(4-(7-(bis((2-(trimethylsilyl)ethoxy)methyl)amino)-3-(quinolin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yloxy)phenyl)acetate (150 mg). HPLC-MS tR=2.60 min (UV254 nm); mass calculated for formula C36H47N5O5Si2 685.3, observed LCMS m/z 686.3 (M+H).

1. temperatureAfter cooled to room temperature
2. filtrationfiltered through celite
3. concentrationAfter concentration
4. customthe crude was purified with column (silica gel, 0˜30% EtOAc/Hexane)