Hydrochloric Acid → 1-(6-methyl-pyridin-2-yl)-2-(3-methyl-3H-[1,2,3]triazolo[4,5-b]pyridin-5-yl)-ethanone

참여 물질

반응 단계

To a stirred solution of 3,5-dimethyl-3H-[1,2,3]triazolo[4,5-b]pyridine of Step B (200 mg, 1.35 mmol), 6-methylpyridine-2-carboxylic acid methoxy-methyl-amide (268 mg, 1.49 mmol), and tetrahydrofuran (5 ml) a 1.0 M solution of lithium hexamethyldisilazide (3.0 ml, 3.0 mmol) was added −78° C. in 10 min. The mixture was warmed up to ambient temperature in 90 min and stirred at the same temperature for 3 h. Methanol (10 ml) and 10% hydrochloric acid (1.5 ml) were added and stirring continued for 18 h. Sodium hydrogen carbonate (5 g) and dichloromethane (10 ml) were added and stirring continued for 10 min. After filtering off solids, the obtained mixture was concentrated. Chromatography on silica gel, eluting with ethyl acetate-hexane (2:3) yielded the title compound (110 mg, 30%).

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