反应详情

温度

150 °C

4-Methyl-5-oxiran-2-yl-2-benzofuran-1(3H)-one (75 mg, 0.394 mmol, 1.2 mmol) and 5-(1-fluoro-2-piperazin-1-ylethyl)-4-methyl-2-benzofuran-1(3H)-one (90 mg, 0.323 mmol, 1.0 eq) were suspended in ethanol (30 ml). The mixture was heated to 150° C. for 30 min under microwave irradiation. The mixture was concentrated and purify by flash column chromatograph (0-10% MeOH/DCM) to afford the expected product 5-(1-fluoro-2-{4-[2-hydroxy-2-(4-methyl-1-oxo-1,3-dihydro-2-benzofuran-5-yl)ethyl]piperazin-1-yl}ethyl)-4-methyl-2-benzofuran-1(3H)-one as well as byproduct 5-(1-(ethyloxy)-2-{4-[2-hydroxy-2-(4-methyl-1-oxo-1,3-dihydro-2-benzofuran-5-yl)ethyl]piperazin-1-yl}ethyl)-4-methyl-2-benzofuran-1(3H)-one.

1. concentrationThe mixture was concentrated
2. custompurify by flash column chromatograph (0-10% MeOH/DCM)