(3-Fluoro-5-phenylmethoxyphenyl)boronic acid → 3-(3-(benzyloxy)-5-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

Participants

Reaction Steps

3-iodo-1H-pyrazolo[3,4-d]pyrimidin-4-amine (6.10 mmol 1.591 g), (3-(benzyloxy)-5-fluorophenyl)boronic acid (4.06 mmol 1.0 g), dppf (0,610 mmol, 338 mg) Potassium phosphate anhydrous (10.16 mmol, 2.157 g) were suspended in dioxane and the mixture was heated at 180 C for 25 min in a Mw reactor then poured in 100 ml of water. The mixture was stirred overnight then filtered on a buchner funnel washing with 30 ml of water. The crude material was purified by chromatography eluting with DCM\ MeOH (80/20) in DCM to give the title compound (450 mg, 1.342 mmol, 33% yield) as a beige solid.

Provenance & Evidence