反应详情

温度

120 °C

To a nitrogen gas purged mixture of 4-chloro-5-(2-methoxyphenyl)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidine (50 mg, 0.13 mmol) and phenyl boronic acid (23.5 mg, 0.192 mmol) in 2 M potassium carbonate (0.192 mL, 0.385 mmol) and tetrahydrofuran (1.0 mL) was added PdCl2(dppf)-CH2Cl2 (10 mg, 0.013 mmol). The reaction was sealed and heated to 120° C. for 20 minutes. Upon cooling, the reaction mixture was diluted with EtOAc and washed with saturated sodium bicarbonate and brine. The organic layer was then dried with sodium sulfate, filtered, and concentrated under reduced pressure. The crude product was purified by silica chromatography eluting with 1-20% ethyl acetate/hexanes to afford 5-(2-methoxyphenyl)-4-phenyl-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidine. LRMS (ESI) calcd for C25H30N3O2Si [M+H]+: 432, found 432.

1. customTo a nitrogen gas purged
2. customThe reaction was sealed
3. temperatureUpon cooling
4. washwashed with saturated sodium bicarbonate and brine
5. dry with materialThe organic layer was then dried with sodium sulfate
6. filtrationfiltered
7. concentrationconcentrated under reduced pressure
8. customThe crude product was purified by silica chromatography
9. washeluting with 1-20% ethyl acetate/hexanes