反应详情

To a stirred solution of [5-(1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine (0.70 g, 1.80 mmol) in dimethylformamide (14 ml) was added cesium carbonate (2 g) followed by methyl bromoacetate (2551 μl, 2.70 mmol). The mixture was stirred for 18 hours at room temperature, and partitioned between ethyl acetate and water. The aqueous phase was extracted with three portions of ethyl acetate, and the combined organic phases dried over magnesium sulfate and concentrated in vacuo to provide a yellow solid. No further purification was required. Yield: 0.51 g, 61%; LCMS method: basic, RT: 3.77 min, MI: 462 [M+1].

1. custompartitioned between ethyl acetate and water
2. extractionThe aqueous phase was extracted with three portions of ethyl acetate
3. dry with materialthe combined organic phases dried over magnesium sulfate
4. concentrationconcentrated in vacuo
5. customto provide a yellow solid
6. customNo further purification