反应详情

温度

120 °C

The mixture of 7-benzylamino-5-chloro-3-isopropylpyrazolo[4,3-d]pyrimidine XVI (100 mg, 0.331 mmol) and 2 mL of 1-(R,S)-(hydroxymethyl)propylamine was heated at 120° C. for 3 hours. The reaction mixture was evaporated to dryness in vacuo and then chromatographed on silica gel. The mixture of chloroform/methanol (97/3) was used as a mobile phase. Yield=83.5%; white syrupy; MS (ES+): 355.3 (100%, M+H+). 1H-NMR (400 MHz, CDCl3): 0.96 t (3H, J=7.2 Hz, CH3CH2), 1.299 d (3H, J=7.1 Hz), 1.307 d (3H, J=7.1 Hz), 1.6 m (2H), 3.20 sept (1H, J=7.1 Hz), 3.55-3.80 m (3H), 4.74 bs (2H), 7.22-7.35 m (5H).

1. customThe reaction mixture was evaporated to dryness in vacuo
2. customchromatographed on silica gel
3. additionThe mixture of chloroform/methanol (97/3)