反应详情

温度

60 °C

A screw cap vial was charged with 2,4-dichloro-5,7-difluoro-3-methylquinoline (500 mg, 2.016 mmol), tetrakis(triphenylphosphine)palladium(0) (233 mg, 0.202 mmol), and THF (5.04 mL). The mixture was sparged with N2, then 3-fluoro-benzylzinc chloride (0.5M in THF, 4.23 mL, 2.116 mmol) was added and the reaction stirred at 60° C. for 2 h. The reaction was then partitioned between EtOAc and water, and the organic layer washed with brine, dried (MgSO4), and concentrated. The crude material was purified by flash chromatography, eluting with a gradient of 0-15% EtOAc in hexane to give 4-chloro-5,7-difluoro-2-(3-fluorobenzyl)-3-methylquinoline. Mass Spectrum (ESI) m/e=322.0 (M+1).

1. customA screw cap vial
2. customThe mixture was sparged with N2
3. customThe reaction was then partitioned between EtOAc and water
4. washthe organic layer washed with brine
5. dry with materialdried (MgSO4)
6. concentrationconcentrated
7. customThe crude material was purified by flash chromatography
8. washeluting with a gradient of 0-15% EtOAc in hexane