反应详情

温度

-78 °C

To a solution of 4-bromo-1-(4-ethylbenzyloxy)-2-methoxybenzene (1.2 g) prepared in (1) in THF (6.0 mL) was added dropwise 1.6 N n-butyllithium/hexane (2.8 mL) at −78° C. under argon atmosphere. The mixture was stirred at −78° C. for 30 min. A solution of 1-Boc-azetidin-3-one (0.64 g) in THF (6.0 mL) was added dropwise over 10 min to the mixture at −78° C. The reaction mixture was allowed to warm to RT and then stirred for 14 hr. Water was added to the reaction mixture and the mixture was extracted with ethyl acetate. The organic layer was dried over MgSO4. The solvent was removed under reduced pressure. The residue was purified by silica gel chromatography (Developing solvent: hexane/ethyl acetate=3/1 to 1/1) to give the title compound (0.88 g, 57%).

1. temperatureto warm to RT
2. stirringstirred for 14 hr
3. extractionthe mixture was extracted with ethyl acetate
4. dry with materialThe organic layer was dried over MgSO4
5. customThe solvent was removed under reduced pressure
6. customThe residue was purified by silica gel chromatography (Developing solvent: hexane/ethyl acetate=3/1 to 1/1)