反应详情

Palladium acetate [Pd(OAc)2] (4 mg, 0.015 mmol), (±)-BINAP (9 mg, 0.015 mmol) and dimethylformamide (1 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-(4-methyl-piperazin-1-yl)-2-trifluoromethoxy-phenylamine (50 mg, 0.18 mmol), 2-(2-iodo-pyrimidin-4-yl)-4-oxo-1-(2,2,2-trifluoro-ethyl)-1,4,6,7-tetrahydro-pyrrolo[3,2-c]pyridine-5-carboxylic acid tert-butyl ester (80 m, 0.15 mmol), and potassium carbonate (205 g, 1.50 mmol) in dimethylformamide (3 mL). The resulting mixture was stirred at 80° C. for 2 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 9/1) to afford 25 mg (25%) 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 2 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 9/1)