反应详情

To a solution of 6-(benzyloxy)-N-(2-fluorophenyl)-3-nitropyridin-2-amine (2.00 g, 5.89 mmol) in dioxane (100 mL) was added Raney nickel (346 mg, 5.89 mmol). The mixture was stirred under hydrogen at room temperature for 12 h, filtered through Celite® and concentrated to give 6-(benzyloxy)-N2-(2-fluorophenyl)pyridin-2,3-diamine as an oil. The residual oil was dissolved in DCM (50 mL) and CDI (629 mg, 3.88 mmol) was added. After stirring at room temperature for 12 h the mixture was concentrated and purified by column chromatography to give the title compound (643 mg). LCMS m/z=336.4 [M+H]+.

1. filtrationfiltered through Celite®
2. concentrationconcentrated