反应详情

3-(3-Amino-1-(3-bromo-4-fluorophenyl)-1H-isoindol-1-yl)phenyl trifluoromethane-sulfonate (Scheme #20, H, 0.083 g, 0.16 mmol), 5-pyrimidinylboronic acid (0.019 g, 0.16 mmol), potassium acetate (0.031 g, 0.31 mmol), 1,1′-bis(diphenylphosphino)ferrocene-palladium(II) dichloride dichloromethane (0.006 g, 7.84 μmol) and solvent (2 mL of a mixture of dimethoxyethene and water in a ratio of 4:1) was irradiated under argon atmosphere in a microwave at 130° C. for 20 minutes. When cooled to ambient temperature the mixture was partitioned between ethylacetate and water, the organic phase was dried over magnesium sulfate and evaporated. Purification by preparative HPLC afforded 0.031 g (37%) of the title compound. 1H NMR (CDCl3) δ 9.18 (s, 1 H), 8.86 (d, J=1.26 Hz, 2 H), 7.58-7.45 (m, 4 H), 7.43-7.31 (m, 4 H), 7.30-7.25 (m, 1 H), 7.19-7.10 (m, 2 H), 5.43 (br s, 2 H); MS (ES) m/z 529 [M+1]+.

1. customwas partitioned between ethylacetate and water
2. dry with materialthe organic phase was dried over magnesium sulfate
3. customevaporated
4. customPurification by preparative HPLC