反应详情

温度

90 °C

The mixture of 5-bromo-2-piperidin-4-yl-1H-benzoimidazole (200 mg, 0.53 mol), cyclopropanylboronic acid (58.4 mg, 0.687 mmol), K3PO4 (391 mg, 1.85 mmol), Pd (OAc)2 (6.8 mg, 0.005 mmol) and tricyclohexylphosphine (14.9 mg, 0.053 mmol) in toluene (10 mL) and H2O (3 mL) was stirred at 90° C. under N2 for 12 h. Then it was poured into H2O and extracted with ethyl acetate. The organic layer was dried over Na2SO4 and concentrated to give the crude product which was purified by column chromatography (ethyl acetate:petroleum ether=1:2) to give the compound 5-Cyclopropyl-2-piperidin-4-yl-1H-benzoimidazole (58 mg, 30%) as white solid.

1. extractionextracted with ethyl acetate
2. dry with materialThe organic layer was dried over Na2SO4
3. concentrationconcentrated
4. customto give the crude product which
5. customwas purified by column chromatography (ethyl acetate:petroleum ether=1:2)