反应详情

温度

150 °C

A mixture of 6-bromo-2-(2-cyclopropylpyrimidin-4-yl)-1H-imidazo[4,5-b]pyrazine (86 mg, 0.3 mmol), (R)-piperidin-3-yl(pyrrolidin-1-yl)methanone (95 mg, 0.4 mmol), potassium carbonate (98.4, 0.7 mmol), cesium fluoride (124 mg, 0.8 mmol) and diglyme (1.0 mL) was heated to 150° C. for 3 days. The mixture was diluted with water and aqueous hydrochloric acid (1N). The mixture was extracted with ethyl acetate (3×). The combined organics were washed with brine, dried over sodium sulfate, and concentrated under reduced pressure. The residue was purified via HPLC to afford the title compound. MS (ESI+) (M+H) 419.3, HPLC retention time 2.44 min (Method A).

1. extractionThe mixture was extracted with ethyl acetate (3×)
2. washThe combined organics were washed with brine
3. dry with materialdried over sodium sulfate
4. concentrationconcentrated under reduced pressure
5. customThe residue was purified via HPLC