反应详情

温度

100 °C

In a microwave vial methyl 2-((S)-6-((R)-7-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,3-dihydro-1H-inden-1-yloxy)-2,3-dihydrobenzofuran-3-yl)acetate (250 mg), 3-(4-bromo-3,5-dimethylphenoxy)-2,2-dimethylpropan-1-ol (226 mg), K3PO4 (230 mg) are suspended in toluene (2 mL) and water (200 μL) and purged for 10 minutes with argon. Palladium-(II)-acetate (12 mg) and dicyclohexyl(2′,6′-dimethoxybiphenyl-2-yl)phosphine (S-Phos) (44 mg) are added, the vial is sealed and the mixture is stirred at 100° C. for 12 hours. After cooling to room temperature the mixture is partitioned between ethyl acetate and water. The organic phase is washed with brine, dried (MgSO4) and concentrated. The residue is chromatographed on silica gel (cyclohexane/ethyl acetate 99:1→60:40) to give the title compound. Yield: 99 mg; LC (method 8): tR=0.87 min; Mass spectrum (ESI+): m/z=549 [M+H]+.

1. customwater (200 μL) and purged for 10 minutes with argon
2. additionPalladium-(II)-acetate (12 mg) and dicyclohexyl(2′,6′-dimethoxybiphenyl-2-yl)phosphine (S-Phos) (44 mg) are added
3. customthe vial is sealed
4. temperatureAfter cooling to room temperature the mixture
5. customis partitioned between ethyl acetate and water
6. washThe organic phase is washed with brine
7. dry with materialdried (MgSO4)
8. concentrationconcentrated
9. customThe residue is chromatographed on silica gel (cyclohexane/ethyl acetate 99:1→60:40)