反应详情

温度

120 °C

The mixture of 2-azetidin-3-yl-5-methyl-1H-benzoimidazole (450 mg, 2.4 mmol), 3,4,5-trichloro-pyridine (438 mg, 2.4 mmol) and Et3N (969 mg, 9.6 mmol) in DMSO (20 ml) was heated at 120° C. under microwave for 1.5 h. Then it was diluted with DCM and H2O. The organic layers were concentrated to give the title compound which was purified by column chromatography and followed by preparative HPLC to afford the pure product 2-[1-(3,5-dichloro-pyridin-4-yl)-azetidin-3-yl]-5-methyl-1H-benzoimidazole (800 mg, yield 55%). [M+1] 333. IC50 (uM) 0.21.

1. concentrationThe organic layers were concentrated