反应详情

温度

100 °C

A mixture of 2-(((2S,3R)-1-(4-fluoro-2-iodobenzoyl)-3-methylpiperidin-2-yl)methyl)isoindoline-1,3-dione (0.51 g, 1.0 mmol), 2-(tributylstannyl)pyrimidine (0.406 g, 1.1 mmol), CsF (0.304 g, 2.0 mmol), CuI (0.019 g, 0.1 mmol) and Pd(PPh3)4 (0.116 g, 0.1 mmol) in DMF (5 mL) was degassed and heated at 100° C. for 16 h. The solvent was removed in vacuo to obtain the crude which was purified by silica gel chromatography (0˜100% EtOAc/hexanes) to yield the title compound as a white solid (0.370 g, 81%). MS (ESI) 459 (M+H).

1. customwas degassed
2. customThe solvent was removed in vacuo
3. customto obtain the crude which
4. customwas purified by silica gel chromatography (0˜100% EtOAc/hexanes)