反应详情

Palladium acetate [Pd(OAc)2] (60 mg, 0.271 mmol), (±)-BINAP (169 mg, 0.271 mmol) and dimethylformamide (15 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 2-methoxy-4-(4-methyl-piperazin-1-yl)-phenylamine (600 mg, 2.712 mmol), 5-(2-iodo-pyrimidin-4-yl)-1-methyl-1H-pyrrole-3-carboxylic acid ethyl ester (484 mg, 1.356 mmol), and potassium carbonate (1.87 g, 13.56 mmol) in dimethylformamide (15 mL). The resulting mixture was stirred at 80° C. for 4 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: dichloromethane/methanol 95/5) to afford 160 mg (26%) 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 4 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: dichloromethane/methanol 95/5)