反应详情

温度

140 °C

To a solution of tert-butyl {3-[(2-chloro-7-{[2-(trimethylsilyl)ethoxy]methyl}-7H-pyrrolo[2,3-d]pyrimidin-4-yl)oxy]phenyl}carbamate (300 mg, 0.61 mmol) in 1,4-dioxane (4 mL) in a microwave vial was added 1-[2-(dimethylamino)ethyl]-1H-pyrazol-4-amine (94.1 mg, 0.61 mmol) followed by Cs2CO3 (298 mg, 0.915 mmol), Pd2(dba)3 (8.2 mg, 0.009 mmol) and Xantphos (5.4 mg, 0.009 mmol) and the mixture heated in the microwave to 140° C. for 45 min. The reaction was cooled to rt and brine (20 mL) was added and the mixture was extracted with EtOAc (three×10 mL). The combined extracts were dried over MgSO4, filtered and stripped to give the title compound as a dark oil that was taken on to the next step with no purification. m/z (ESI+) for C30H44N8O4Si 609.25 (M+H)+.

1. temperatureThe reaction was cooled to rt
2. extractionthe mixture was extracted with EtOAc (three×10 mL)
3. dry with materialThe combined extracts were dried over MgSO4
4. filtrationfiltered