反应详情

温度

80 °C

A mixture of 3-bromo-2-(6-methyl-pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole (99 mg, 0.36 mmol), 3,4-methylenedioxyphenylboronic acid (65 mg, 0.39 mmol), (PPh3)4Pd (20 mg, 0.02 mmol), 1 N aqueous sodium carbonate solution (500 μL, 0.5 mmol) in toluene (5 mL) and methanol (1 mL) is purged with argon for 10 min and heated at 80° C. under nitrogen for 30 h. The mixture is cooled and partitioned between water and ethyl acetate, and the organic portion washed with water and brine, dried (sodium sulfate), filtered, and concentrated in vacuo. The crude residue is chromatographed on SiO2 (ethyl acetate) to yield the title compound, 10 mg (9%), as a yellow solid.

1. customis purged with argon for 10 min
2. temperatureThe mixture is cooled
3. custompartitioned between water and ethyl acetate
4. washthe organic portion washed with water and brine
5. dry with materialdried (sodium sulfate)
6. filtrationfiltered
7. concentrationconcentrated in vacuo
8. customThe crude residue is chromatographed on SiO2 (ethyl acetate)