反应详情

温度

80 °C

A solution of pyrrolidine (50 mL, 0.6 mmol) in toluene (2 mL) was treated with a solution of phosgene in toluene (0.31 mL, 1.93-M, 0.6 mmol), heated at 80° C. for 30 mins, cooled and concentrated in vacuo. The residue was dissolved in THF (2 mL) and added to a solution of 6-(2-furyl)-1H-purine-2-amine (100 mg, 0.5 mmol) and Et3N (83 mL, 0.6 mmol) in DMP (0.5 mL), stirred at 60° C. for 16 h, poured into water and extracted with EtOAc. The combined organic phase was dried (MgSO4), concentrated in vacuo and the resulting solid triturated with EtOAc/heptane and filtered to give the title compound (92 mg, 62%) as a cream solid.

1. temperaturecooled
2. concentrationconcentrated in vacuo
3. dissolutionThe residue was dissolved in THF (2 mL)
4. extractionextracted with EtOAc
5. dry with materialThe combined organic phase was dried (MgSO4)
6. concentrationconcentrated in vacuo
7. customthe resulting solid triturated with EtOAc/heptane
8. filtrationfiltered