反应详情

温度

80 °C

A flask was charged with trifluoro-methanesulfonic acid 2-(2-methoxy-phenyl)-5-(2,2,6,6-tetramethyl-tetrahydro-pyran-4-yl)-2H-pyrazol-3-yl ester (354 mg, 0.69 mmol) (Example 1, step E),4-(benzyloxy)phenylboronic acid (238.3 mg, 1.0 mmol), tetrakis(triphenylphosphine)palladium(0) (40 mg, 0.035 mmol), 2M Na2CO3 (2.8 mL) and 2:1 toluene/ethanol (10 mL) and the mixture was heated at 80° C. for 6 hrs. The resulting mixture was diluted with EtOAc and washed with sat. NaCl. EtOAc was removed under vacuum and the residue was purified by silica column chromatography to give 257.8 mg (74.5%) of the title compound.

1. washwashed with sat. NaCl
2. customEtOAc was removed under vacuum
3. customthe residue was purified by silica column chromatography