反应详情

3-(1-(4-amino-3-iodo-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-4-(3-(4,4,5,5-tetramethyl-1,3-dioxolan-2-yl)phenyl)-1H-isochromen-1-one (Intermediate D8, 1.14 g, 1.788 mmol), (3-fluoro-5-hydroxyphenyl)boronic acid (0.558 g, 3.58 mmol), K2CO3 (0.494 g, 3.58 mmol) and PdCl2(dppf) (0.196 g, 0.268 mmol) were reacted in dioxane (30 ml) overnight at 120° C. The reaction was diluted with DCM (100 ml), filtered to remove solids, and the filtrate evaporated under reduced pressure. The crude was purified via flash chromatography on silica gel using a Biotage 100G SNAP with a gradient of DCM and MeOH to give the title compound (819 mg, 73.7%) as brown pale solid.

1. filtrationfiltered
2. customto remove solids
3. customthe filtrate evaporated under reduced pressure
4. customThe crude was purified via flash chromatography on silica gel using a Biotage 100G SNAP with a gradient of DCM and MeOH