反应详情

温度

80 °C

The mixture of 4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-pyrazole (1.0 g, 5.0 mmol), 1-[1-(2,4-dimethoxybenzyl)-5-oxopyrrolidin-3-yl]ethyl methanesulfonate (1.5 g, 4.2 mmol), NaI (64.0 mg, 0.04 mmol) and K2CO3 (1.2 g, 8.4 mmol) in DMF (15 mL) was stirred at 80° C. for 8 hours. The mixture was then diluted with water and extracted with EtOAc. The EtOAc layer was dried over sodium sulfate and concentrated under reduced pressure to afford racemic 1-(2,4-dimethoxybenzyl)-4-{1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl]ethyl}pyrrolidin-2-one which was used in next step without purification. MS ESI calc'd. for C24H35BN3O5 [M+H]+ 456. found 456.

1. extractionextracted with EtOAc
2. dry with materialThe EtOAc layer was dried over sodium sulfate
3. concentrationconcentrated under reduced pressure