反应详情

Palladium acetate [Pd(OAc)2] (0.12 g, 0.55 mmol), (±)-BINAP (0.34 g, 0.55 mmol) and dimethylformamide (60 mL) were charged to a round-bottom flask flushed with argon. The flask was evacuated and backfilled with argon. The mixture was stirred under argon for 30 minutes and added to a mixture of 5-bromo-2-trifluoromethoxy aniline (2.0 g, 5.60 mmol), 5-(2-iodo-pyrimidin-4-yl)-1-methyl-1H-pyrrole-3-carboxylic acid ethyl ester (1.44 g, 5.60 mmol), and potassium carbonate (7.70 g, 55.80 mmol) in dimethylformamide (90 mL). The resulting mixture was stirred at 80° C. for 3 hours under argon. After cooling to room temperature, the reaction mixture was filtered on a pad of celite. The solvent was concentrated, the crude solid was purified by flash chromatography on silica gel (eluant: hexane/ethyl acetate 70/30) to afford 1.41 g (52%) of the title compound as white solid.

1. customflushed with argon
2. customThe flask was evacuated
3. stirringThe resulting mixture was stirred at 80° C. for 3 hours under argon
4. filtrationthe reaction mixture was filtered on a pad of celite
5. concentrationThe solvent was concentrated
6. customthe crude solid was purified by flash chromatography on silica gel (eluant: hexane/ethyl acetate 70/30)