反应详情

To the solution of 5-chloro-2-(1-cyclohexylmethyl-5,6-difluoro-1H-benzoimidazol-2-yl)-phenol (Example 19, intermediate a) (98 mg, 0.26 mmol) in acetone (10 ml) was added cesium carbonate (127 mg, 0.39 mmol) followed by bromomethyl-cyclohexane (42 mg, 0.31 mmol; CAS Reg. No. 2550-36-9) and the reaction was refluxed for 12 h. The reaction mixture was filtered, and the filtrate was concentrated under reduced pressure. The crude material was purified by column chromatography using silica gel (30-40% ethyl acetate/n-hexane) to afford the desired product as an off-white powder (56%). MS (Turbo Spray): m/z=473.0 (M+H).

1. temperature2550-36-9) and the reaction was refluxed for 12 h
2. filtrationThe reaction mixture was filtered
3. concentrationthe filtrate was concentrated under reduced pressure
4. customThe crude material was purified by column chromatography