反应详情

温度

100 °C

2,6-Dichloropyrimidin-4-amine (0.2 g, 1.22 mmol), tetrakis(triphenylphosphine)palladium(0) (42 mg, 0.043 mmol) and copper iodide (14 mg, 0.07 mmol) were introduced in a flask. A mixture of THF-triethylamine 2:3 (5 mL) was added and the system was inertized 3 times with vacuum/argon cycles. Finally, cyclopentyl acetylene (0.16 mL, 1.34 mmol) was added and the resulting mixture was heated at 100° C. overnight. The reaction crude was cooled at room temperature and filtered over Celite®. The solvent was evaporated to dryness and the residue was purified by chromatography over silica gel using mixtures of hexane/EtOAc of increasing polarity as eluent, providing 0.15 g of the title compound, impurified with its regioisomer.

1. additionwas added
2. customThe reaction crude
3. temperaturewas cooled at room temperature
4. filtrationfiltered over Celite®
5. customThe solvent was evaporated to dryness
6. customthe residue was purified by chromatography over silica gel using mixtures of hexane/EtOAc
7. temperatureof increasing polarity as eluent