反应详情

5-Bromo-2-(piperidin-1-yl)pyridin-3-amine (0.0537 g, 0.210 mmol), 4-chloro-5,7-difluoro-3-methyl-2-(pyridin-2-yl)quinoline (0.0632 g, 0.217 mmol), and hydrochloric acid, 4.0M in 1,4-dioxane (0.05 mL, 0.200 mmol) were stirred in NMP (0.50 mL) then microwaved at 150° C. After an additional 4 h, the reaction was diluted with EtOAc and washed once with satd aq. sodium bicarbonate and once with brine. After drying over anhydrous sodium sulfate, filtration, and concentration, the brown residue was purified with silica gel chromatography (0-40% EtOAc in hexanes) to yield mostly N-(5-bromo-2-(piperidin-1-yl)pyridin-3-yl)-5,7-difluoro-3-methyl-2-(pyridin-2-yl)quinolin-4-amine. Mass Spectrum (ESI) m/e=510.2 (M+1).

1. customthen microwaved at 150° C
2. washwashed once with satd aq. sodium bicarbonate and once with brine
3. dry with materialAfter drying over anhydrous sodium sulfate, filtration, and concentration
4. customthe brown residue was purified with silica gel chromatography (0-40% EtOAc in hexanes)