反应详情

温度

90 °C

A mixture of 6-(4-fluoro-phenyl)-3-iodo-pyrazolo[1,5-a]pyridine (140 mg, 0.41 mmol) and 3-aminophenylboronic acid pinacol ester (120 mg, 0.5 mmol) in DME (2 ml) and 2N Na2CO3 (aq, 2 ml) was deoxygenated by evacuation/refill with N2 (×3). PdCl2ddpf (15 mg, 0.02 mmol) was added and the mixture was deoxygenated again (×2). The reaction was stirred and heated at 90° C. under N2 for 24 hours. After cooling to RT the mixture was partitioned between CH2Cl2/H2O. The layers were separated using a phase separating cartridge. The organic layer was evaporated and the residue was purified by chromatography on silica (25→65% EtOAc/Petrol) to give the title compound (55 mg, solid).

1. customwas deoxygenated by evacuation/refill with N2 (×3)
2. additionPdCl2ddpf (15 mg, 0.02 mmol) was added
3. customthe mixture was deoxygenated again (×2)
4. temperatureAfter cooling to RT the mixture
5. customwas partitioned between CH2Cl2/H2O
6. customThe layers were separated
7. customseparating cartridge
8. customThe organic layer was evaporated
9. customthe residue was purified by chromatography on silica (25→65% EtOAc/Petrol)