反应详情

温度

130 °C

To a nitrogen gas purged mixture of 4-chloro-5-iodo-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidine (200 mg, 0.488 mmol), and (2-methoxyphenyl)boronic acid (96 mg, 0.64 mmol) in 2 M aqueous sodium carbonate (0.610 mL, 1.22 mmol) and DME (3.0 mL) was added tetrakis(triphenylphosphine)palladium(0) (56 mg, 0.049 mmol). The reaction was sealed and heated at 130° C. for 30 minutes. The reaction was then diluted with EtOAc and passed through a column of Celite and sodium sulfate to remove water and solids. The reaction solution was concentrated under reduced pressure and the crude product purified by silica chromatography eluting with 1-20% ethyl acetatehexane to afford 4-chloro-5-(2-methoxyphenyl)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidine as a solid. LRMS (ESI) calcd for C19H25ClN3O2Si [M+H]+: 390, found 390.

1. customTo a nitrogen gas purged
2. customThe reaction was sealed
3. customto remove water and solids
4. concentrationThe reaction solution was concentrated under reduced pressure
5. customthe crude product purified by silica chromatography
6. washeluting with 1-20% ethyl acetatehexane