反应详情

A vial was charged with 2,4-dichlorofuro[3,2-d]pyrimidine (0.50 g, 2.6 mmol, Ark Pharm), TEA (0.369 mL, 2.65 mmol), 1,4-dioxane (20 mL) and cyclopropylamine (0.186 mL, 2.65 mmol). The mixture was stirred at rt for about 5 h and then passed through a 5.0 g SiCO3 SPE cartridge, (MeOH eluent) and concentrated under reduced pressure. The residue was purified by silica gel chromatography with a gradient of 0 to 50% EtOAc/hexanes to give 2-chloro-N-cyclopropylfuro[3,2-d]pyrimidin-4-amine (0.5 g, 90%). 1H NMR (CDCl3): δ 7.77 (s, 1H); 6.80 (s, 1H), 5.51 (s, 1H) 3.07 (m, 1H) 0.96 (q, J=5 Hz, 15 Hz, 2H) 0.70, (q, J=5 Hz, 15 Hz, 2H).

1. concentrationconcentrated under reduced pressure
2. customThe residue was purified by silica gel chromatography with a gradient of 0 to 50% EtOAc/hexanes