反应详情

N-tert-Butyl-2-(5-(difluoromethoxy)-1H-indazol-3-yl)-5-((2-(trimethylsilyl)ethoxy)methyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide (100 mg, 188 μmol), 4-benzyl-2-(chloromethyl)morpholine (51.0 mg, 226 μmol) and cesium carbonate (184 mg, 565 mmol) in dimethylformamide (1.4 mL) were heated in a microwave at 100° C. for 45 min. The mixture was cooled, partitioned between ethyl acetate and water, and the organic phases combined and washed with water 3 times. The organic phase was dried and concentrated in vacuo. Purification by chromatography (silica, 24 g Analogix column, 0-40% ethyl acetate in hexanes) gave 2-(1-((4-benzylmorpholin-2-yl)methyl)-5-(difluoromethoxy)-1H-indazol-3-yl)-N-tert-butyl-5-((2-(trimethylsilyl)ethoxy)methyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide (67 mg, 49%).

1. temperatureThe mixture was cooled
2. custompartitioned between ethyl acetate and water
3. washwashed with water 3 times
4. customThe organic phase was dried
5. concentrationconcentrated in vacuo
6. customPurification by chromatography (silica, 24 g Analogix column, 0-40% ethyl acetate in hexanes)