反应详情

To a solution of 5-(4-bromophenyl)-5H-imidazo[2,1-a]isoindole (3.17 g) in THF (60 mL) at −78° C. was added LAD solution (10.19 mL, 1.5 M in cyclohexane) drop wise. After stirring for 5 minutes tert-butyl bromoacetate was added, cooling bath was removed and the reaction mixture was stirred at room temperature. After 1.5 h the reaction was quenched with aqueous saturated NH4Cl and layers were separated. Aqueous layer was extracted with EtOAc (2×). Combined organic layers were dried over Na2SO4 and concentrated. Flash chromatography using a linear gradient of 1-50% EtOAc in hexanes afforded title compound as a white solid. Mass. found (M+H)+, 427.0.

1. additionwas added
2. temperaturecooling bath
3. customwas removed
4. customAfter 1.5 h the reaction was quenched with aqueous saturated NH4Cl and layers
5. customwere separated
6. extractionAqueous layer was extracted with EtOAc (2×)
7. dry with materialCombined organic layers were dried over Na2SO4
8. concentrationconcentrated