反应详情

The mixture 138 mg of 7-benzylamino-5-chloro-3-isopropylpyrazolo[4,3-d]pyrimidine (XVI), 0.62 mL of 2-aminoethylamine (20 eq.) and 0.6 mL of N-methyl-2-pyrrolidone was heated at 125° C. for 12 hours. The reaction mixture was evaporated to dryness in vacuo and then chromatographed over silica gel. The mixture of chloroform/methanol/NH4OH (91:9:1) was used as a mobile phase. Yield=56%; mp=145-147° C.; MS (ES+): 326.1 (100%, M+H+). 1H-NMR (300 MHz, CD3OD): 1.41 d (6H, J=6.9 Hz), 3.10 t (2H, J=5.8 Hz), 3.35 sept (1H, J=6.9 Hz), 3.73 t (2H, 5.8 Hz), 4.86 s (2H), 7.34 m (5H).

1. customThe reaction mixture was evaporated to dryness in vacuo
2. customchromatographed over silica gel
3. additionThe mixture of chloroform/methanol/NH4OH (91:9:1)