反应详情

A mixture of methyl 5-(benzyloxy)-2-bromo-2′,4′-difluorobiphenyl-4-carboxylate (34.3 g), cyclopropylboronic acid (17.0 g), dicyclohexyl(2′,6′-dimethoxybiphenyl-2-yl)phosphine (4.87 g), a 2 M aqueous sodium carbonate solution (119 mL), tris(dibenzylideneacetone)dipalladium(0) (5.07 g), and toluene (150 mL) was stirred overnight at 100° C. The reaction mixture was poured to water at room temperature, followed by extraction with ethyl acetate. The obtained organic layer was washed with saturated saline and passed through a short silica gel (NH) column, and the solvent was distilled off under reduced pressure. The obtained residue was purified by silica gel column chromatography (hexane/ethyl acetate) to obtain the title compound (20.3 g).

1. extractionfollowed by extraction with ethyl acetate
2. washThe obtained organic layer was washed with saturated saline
3. distillationthe solvent was distilled off under reduced pressure
4. customThe obtained residue was purified by silica gel column chromatography (hexane/ethyl acetate)