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 (170 mg) and 3-((4-bromo-3,5-dimethylphenoxy)methyl)tetrahydrofuran (170 mg) and K3PO4 (290 mg) are suspended in tetrahydrofuran (10 mL). The mixture is purged for 5 minutes with argon. [1,1′-Bis(diphenylphosphino)-ferrocene]-dichloropalladium (27 mg) is added, the vial is sealed and the mixture is stirred at 100° C. for 12 hours. After cooling to room temperature the mixture is diluted with diethylether and washed with saturated aqueous NH4Cl solution. The organic phase is dried (MgSO4) and concentrated. The residue is chromatographed on silica gel (cyclohexane/ethyl acetate 90:10→50:50) to give the title compound. Yield: 47 mg; LC (method 1): tR=1.48 min; Mass spectrum (ESI+): m/z=569 [M+Na]+.

1. customThe mixture is purged for 5 minutes with argon
2. addition[1,1′-Bis(diphenylphosphino)-ferrocene]-dichloropalladium (27 mg) is added
3. customthe vial is sealed
4. temperatureAfter cooling to room temperature the mixture
5. additionis diluted with diethylether
6. washwashed with saturated aqueous NH4Cl solution
7. dry with materialThe organic phase is dried (MgSO4)
8. concentrationconcentrated
9. customThe residue is chromatographed on silica gel (cyclohexane/ethyl acetate 90:10→50:50)