反应详情

温度

100 °C

To a solution of (R)-methyl-3-(5-methoxypyridin-2-ylamino)-2-(oxiran-2-ylmethoxy)benzoate 0.53 g (1.6 mmol) of step 5 in dimethylformamide 5 mL was added K2CO3 0.28 g (2.0 mmol), followed by stirring at 100° C. for 5 hrs. The reaction mixture is cooled to room temperature, concentrated in a vacuum, diluted with ethylacetate, and washed with distilled water and a saturated NaCl solution. After drying over magnesium sulfate and concentration in a vacuum, purification by column chromatography (developing solvent: ethylacetate/hexane=1/1) afforded 0.50 g of the title compound (yield 94%).

1. temperatureThe reaction mixture is cooled to room temperature
2. concentrationconcentrated in a vacuum
3. additiondiluted with ethylacetate
4. washwashed with distilled water
5. dry with materialAfter drying over magnesium sulfate and concentration in a vacuum, purification by column chromatography (developing solvent: ethylacetate/hexane=1/1)