反应详情

温度

120 °C

Cesium carbonate (4.68 g, 14.4 mmol), 2-chloroquinoline (0.782 g, 4.8 mmol) and tert-butyl azetidin-3-yl-carbamate hydrochloride (1.0 g, 4.8 mmol) were dissolved in dry dimethylformamide (15 mL) and the resulting mixture was heated at 120° C. overnight. The mixture was diluted with water (40 mL) and extracted with ethyl acetate (2×50 mL). The combined organic extracts were washed with water (30 mL) and brine (30 mL), then dried over sodium sulfate. The organic was evaporated in vacuo and the residue was purified by flash column chromatography on silica gel (20% to 40% ethyl acetate in petroleum ether) to give tert-butyl (1-(quinolin-2-yl)azetidin-3-yl)-carbamate (1.14 g, 3.84 mmol, 80% yield) as white solid.

1. extractionextracted with ethyl acetate (2×50 mL)
2. washThe combined organic extracts were washed with water (30 mL) and brine (30 mL)
3. dry with materialdried over sodium sulfate
4. customThe organic was evaporated in vacuo
5. customthe residue was purified by flash column chromatography on silica gel (20% to 40% ethyl acetate in petroleum ether)