反应详情

温度

95 °C

3-Bromo-1-(tetrahydro-2-pyranyl)-1H-indazole-5-carbonitrile (1.00 g, 3.27 mmol), 2-benzofuranboronic acid (795 mg, 4.90 mmol), Pd(dppf)Cl2.CH2Cl2 (266 mg) and potassium phosphate (3.47 g, 16.35 mmol) in 1,2-dimethoxyethane (16.0 mL) was placed into a screw-top pressure tube and heated in a 95° C. oil bath for 21 h. The reaction mixture was cooled and partitioned between dichloromethane and water. The organic layer was separated, washed with satd. NaHCO3, brine, dried over MgSO4 and concentrated in vacuo to give a residue which was purified by flash chromatography on silica gel with 30% ethyl acetate in hexane (R=0.49) to afford the desired product (167 mg, 15% yield) as a pale orange foam.

1. temperatureThe reaction mixture was cooled
2. custompartitioned between dichloromethane and water
3. customThe organic layer was separated
4. washwashed with satd
5. dry with materialNaHCO3, brine, dried over MgSO4
6. concentrationconcentrated in vacuo
7. customto give a residue which
8. customwas purified by flash chromatography on silica gel with 30% ethyl acetate in hexane (R=0.49)