反应详情

温度

90 °C

In a 250 mL round bottom flask, added 6-Bromo-pyridin-3-ol (4.69 g, 26.95 mmol) and 3-Iodo-azetidine-1-carboxylic acid tert-butyl ester (7.63g, 26.95 mmol) and Cs2CO3 (12.26 g, 37.73 mmol) in DMF (10 mL) with stirring under argon. The reaction was heated at 90° C. overnight. Reaction was then poured onto water (200 mL). The crude product was extracted with EtOAc (3×50 mL). The organic extraction was concentrated and purified by flash chromatography with 10% EtOAc in Hexanes to afford product 2.62 g (yield 30%) of 3-(6-Bromo-pyridin-3-yloxy)-azetidine-1-carboxylic acid tert-butyl ester as light brown solid.

1. customReaction
2. additionwas then poured onto water (200 mL)
3. extractionThe crude product was extracted with EtOAc (3×50 mL)
4. extractionThe organic extraction
5. concentrationwas concentrated
6. custompurified by flash chromatography with 10% EtOAc in Hexanes