反应详情

DMF/water (4:1, 2 mL) was added to a mixture of tert-butyl 4-(3-bromo-1-(pyridin-4-yl)-1H-indol-6-yl)piperazine-1-carboxylate (29 mg, 0.0636 mmol), potassium carbonate (18 mg, 0.13 mmol) and 4-methoxyphenylboronic acid (11 mg, 0.070 mmol) and the dissolved gas was removed. After adding Pd(dppf)Cl2 (10.4 mg, 0.013 mmol), the mixture was stirred at room temperature for 14 hours. After adding ethyl acetate and water, the mixture was filtered using a diatomite pad. After separation of the organic layer, the aqueous layer was extracted with ethyl acetate. The collected organic layer was washed with brine and concentrated under reduced pressure by drying with anhydrous magnesium sulfate. The residue was purified by chromatography (silica gel, EA:Hx=1:4 1:1). The target compound (31 mg) was obtained as white solid.

1. customthe dissolved gas was removed
2. filtrationthe mixture was filtered
3. customAfter separation of the organic layer
4. extractionthe aqueous layer was extracted with ethyl acetate
5. washThe collected organic layer was washed with brine
6. concentrationconcentrated under reduced pressure
7. dry with materialby drying with anhydrous magnesium sulfate
8. customThe residue was purified by chromatography (silica gel, EA:Hx=1:4 1:1)