反应详情

(6-(3,5-dimethylisoxazol-4-yl)-2-ethoxy-1H-benzo[d]imidazol-4-yl)(pyridin-2-yl)methanone (40 mg, 0.11 mmol) was dissolved in dry THF (1.1 mL) and cyclopropylmagnesium bromide (0.5 M in diethylether, 1.1 mL, 0.55 mmol) was added dropwise at rt and the reaction was allowed to stir for 10 minutes. The reaction was quenched with water, concentrated, and purified by reverse-phase HPLC to give cyclopropyl(6-(3,5-dimethylisoxazol-4-yl)-2-ethoxy-1H-benzo[d]imidazol-4-yl)(pyridin-2-yl)methanol intermediate which was taken up in 1.0 mL EtOH and 0.7 mL 4.0M HCl/dioxane and heated for 2 hours at 65° C. Reaction was then concentrated down and purified by reverse-phase HPLC to afford the desired product as a white powder.

1. customThe reaction was quenched with water
2. concentrationconcentrated
3. custompurified by reverse-phase HPLC