反应详情

温度

120 °C

3-(1-(4-amino-3-iodo-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-4-phenyl-1H-isochromen-1-one (Intermediate D2a, 60 mg, 0.118 mmol), K2CO3 (32.6 mg, 0.236 mmol), 2-aminopyrimidin-5-ylboronic acid (32.7 mg, 0.236 mmol) and Pd(dppf)Cl2 (4.31 mg, 5.89 μmol) were reacted in 2 ml of dioxane, purged with argon and heated overnight at 120° C. The reaction was quenched by the addition of 1M HClaqueous (2 ml) and the resulting mixture was straightforward purified via reverse phase chromatography using a Biotage C18 30 g SNAP with a gradient of water and acetonitrile (prior to drying 2 ml of 1M HClaqueous were added) to give the title compound (16.2 mg, 28.9%) as a yellow solid.

1. custompurged with argon
2. customThe reaction was quenched by the addition of 1M HClaqueous (2 ml)
3. customthe resulting mixture was straightforward purified via reverse phase chromatography
4. customto drying 2 ml of 1M HClaqueous
5. additionwere added)