反应详情

3-Chloro-5-methyl-2H-isoquinolin-1-one (100 mg, 0.52 mmol), bis(pinacolato)diboron (157 mg, 0.62 mmol), Pd(dppf)Cl2 (42 mg, 0.054 mmol) and KOAc (153 mg, 1.56 mmol) in 1,4-dioxane (2 mL) were added to a microwave vial and the reaction mixture purged with N2 for 10 min. The reaction mixture was irradiated using a microwave reactor (300 W, 120° C., 20 min). The reaction mixture was passed through a Si-thiol cartridge and concentrated in vacuo. The crude product was purified by reverse phase preparative HPLC-MS to afford 5-methyl-1-oxo-1,2-dihydro-isoquinoline-3-boronic acid as a white solid (51 mg, 49%).

1. customthe reaction mixture purged with N2 for 10 min
2. customThe reaction mixture was irradiated
3. custom(300 W, 120° C., 20 min)
4. concentrationconcentrated in vacuo
5. customThe crude product was purified by reverse phase preparative HPLC-MS