反应详情

温度

120 °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 (75 mg), 4-iodo-N,3,5-trimethylbenzamide (93 mg), K3PO4 (102 mg) and dicyclohexyl(2′,6′-dimethoxybiphenyl-2-yl)phosphine (S-Phos) (7 mg) are suspended in toluene (1.8 mL) and water (0.2 mL) and purged for 10 minutes with argon. Palladium-(II)-acetate (4 mg) is added, the vial is sealed and the mixture is stirred at 120° C. for 5 hours. After cooling to ambient temperature the mixture is partitioned between ethyl acetate and water. The organic phase is dried (MgSO4) and concentrated. The residue is chromatographed on silica gel (cyclohexane/ethyl acetate 100:0→80:20) to give the title compound. Yield: 16 mg; LC (method 25): tR=1.32 min; Mass spectrum (ESI+): m/z=504 [M+H]+.

1. customwater (0.2 mL) and purged for 10 minutes with argon
2. additionPalladium-(II)-acetate (4 mg) is added
3. customthe vial is sealed
4. temperatureAfter cooling to ambient temperature the mixture
5. customis partitioned between ethyl acetate and water
6. dry with materialThe organic phase is dried (MgSO4)
7. concentrationconcentrated
8. customThe residue is chromatographed on silica gel (cyclohexane/ethyl acetate 100:0→80:20)