反应详情

温度

70 °C

A mixture of 2,4-dibromothiazole (1.00 g, 4.12 mmol), azetidin-3-ol hydrochloride (0.543 g, 4.96 mmol), and cesium carbonate (4.03 g, 12.37 mmol) in acetonitrile (30 mL) was stirred for 18 h at 70° C. The reaction mixture was cooled to room temperature and filtered. The filtrate was concentrated under vacuum, and the residue was purified via column chromatography on silica gel (eluting with 10:1, dichloromethane/methanol) to afford 1-(4-bromothiazol-2-yl)azetidin-3-ol (0.535 g, 53%) as a light yellow solid. MS (ESI, pos. ion) m/z 235, 237 [M+H]+.

1. temperatureThe reaction mixture was cooled to room temperature
2. filtrationfiltered
3. concentrationThe filtrate was concentrated under vacuum
4. customthe residue was purified via column chromatography on silica gel (eluting with 10:1, dichloromethane/methanol)