反应详情

温度

100 °C

The mixture of 2-[1-(3,5-dichloro-pyridin-4-yl)-azetidin-3-yl]-5-methyl-1H-benzoimidazole (200 mg, 0.60 mol), phenylboronic acid (80 mg, 0.66 mmol), K2CO3 (166 mg, 1.2 mmol) and Pd(dppf)Cl2 (44 mg, 0.06 mmol) in toluene (10 mL) and H2O (3 mL) was stirred at 100° C. under N2 for 12 h. The mixture was then poured into H2O and extracted with ethyl acetate. The organic layer was dried over Na2SO4 and concentrated to give the crude product and purified by column chromatography and followed by preparative HPLC to afford pure product 2-[1-(3-chloro-5-phenyl-pyridin-4-yl)-azetidin-3-yl]-5-methyl-1H-benzoimidazole (30 mg, 14%) as white solid. [M+1] 375. IC50 (uM) 0.022.

1. extractionextracted with ethyl acetate
2. dry with materialThe organic layer was dried over Na2SO4
3. concentrationconcentrated
4. customto give the crude product
5. custompurified by column chromatography