反应详情

3-iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine (1.52 g, 5.82 mmol), 3-fluoro-5-methoxyphenylboronic acid (1.4 g, 8.24 mmol), Pd(dppf)Cl2 (0.18 g, 0.246 mmol) and 8.7 mL of 1M NaOHaqueous (8.73 mmol) were reacted in DMF (13 mL) under Ar at 120° C. for 48 hrs. The reaction was quenched by the addition of 1M HClaqueous (10 mL), dried under reduced pressure and the dark crude oil purified via flash chromatography on silica gel using a Biotage 100G SNAP with a gradient of DCM and iPrOH to give the title compound (275 mg, 18.2%) as yellowish solid.

1. customThe reaction was quenched by the addition of 1M HClaqueous (10 mL)
2. customdried under reduced pressure
3. customthe dark crude oil purified via flash chromatography on silica gel using a Biotage 100G SNAP with a gradient of DCM and iPrOH