反应详情

2-(6-Fluoro-1H-indazol-3-yl)-5-((2-(trimethylsilyl)ethoxy)methyl)-5H-pyrrolo[2,3-b]pyrazine-7-carbaldehyde (225 mg, 547 μmol), tert-butyl 3-(iodomethyl)azetidine-1-carboxylate (162 mg, 547 μmol) and cesium carbonate (534 mg, 1.64 mmol) in dimethylformamide (4 mL) were heated in a microwave at 150° C. for 30 min. The mixture was partitioned between ethyl acetate and water. Then the organic phase was washed with water 3 times, dried and concentrated in vacuo. Purification by chromatography (silica, 24 g Analogix column, 0-40% ethyl acetate in hexanes) gave tert-butyl 3-((6-fluoro-3-(7-formyl-5-((2-(trimethylsilyl)ethoxy)methyl)-5H-pyrrolo[2,3-b]pyrazin-2-yl)-1H-indazol-1-yl)methyl)azetidine-1-carboxylate (202 mg, 64%).

1. customThe mixture was partitioned between ethyl acetate and water
2. washThen the organic phase was washed with water 3 times
3. customdried
4. concentrationconcentrated in vacuo
5. customPurification by chromatography (silica, 24 g Analogix column, 0-40% ethyl acetate in hexanes)