反应详情

温度

70 °C

tert-Butyl 2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-9-iodo-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl)acetate (50 mg, 0.078 mmol) was dissolved in THF (1.0 mL) in a heavy walled sealed microwave tube (0.5-2.0 mL) under N2. Cyclobutylzinc(II) bromide (0.156 mL, 0.078 mmol) and bis(tri-t-butylphosphine)palladium(0) (3.60 mg, 7.04 μmol) were added. The reaction mixture was heated to 70° C. for 2 h, quenched with saturated NaHCO3 and filtered through Celite®. The filtrate was then extracted with EtOAc (3×5 mL). The organic layers were combined and washed with saturated NaCl (10 mL), dried over MgSO4 and filtered. The filtrate was concentrated under reduced pressure. The residue was purified by preparative TLC to provide the title compound as an amber oil (17.3 mg). LCMS m/z=568.8 [M+H]+.

1. customquenched with saturated NaHCO3
2. filtrationfiltered through Celite®
3. extractionThe filtrate was then extracted with EtOAc (3×5 mL)
4. washwashed with saturated NaCl (10 mL)
5. dry with materialdried over MgSO4
6. filtrationfiltered
7. concentrationThe filtrate was concentrated under reduced pressure
8. customThe residue was purified by preparative TLC