反应详情

温度

90 °C

To a solution of phenylboronic acid (0.177 g, 1.45 mmol), 2-(1-(3-bromo-6-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidin-2-yl)ethyl)isoindoline-1,3-dione (Prepared in Example 6, 0.40 g, 0.97 mmol) and potassium carbonate (0.402 g, 2.91 mmol) in a mixture of water (0.5 mL) and dioxane (9 mL) was added dichloro 1,1′-bis(diphenylphosphino)ferrocene palladium (II) (0.040 g, 0.049 mmol) under an argon atmosphere. The mixture was stirred at 90° C. for 3 h then was loaded onto silica gel and purified by MPLC (eluted with a gradient of 0-3% MeOH in DCM) to afford 2-(1-(6-methyl-4-oxo-3-phenyl-4H-pyrido[1,2-a]-pyrimidin-2-yl)ethyl)isoindoline-1,3-dione as a yellow solid. Mass Spectrum (ESI) m/e=410.1 (M+1).

1. custompurified by MPLC (
2. washeluted with a gradient of 0-3% MeOH in DCM)