反应详情

3-(3-Cyclopentyloxy-4-methoxy-benzyl)-8-isopropyl-hypoxanthine (5.74 g, 15 mmole) and phosphorus oxychloride (60 ml) were heated to 65° C. for 30 minutes. The reaction mixture was evaporated to dryness in vacuo and the residue evaporated twice with toluene. The crude chloropurine (15 mmole) was dissolved in THF (80ml ) and 32% aqueous ammonia solution (36.2 ml) and heated together with liquid ammonia (50 g) in a 450 ml pressure reactor to 60° C. (340 psi) for 4 hours. The solvents were evaporated in vacuo and the residue suspended in a mixture of diethyl ether and 1 M NaOH solution. The solid was collected and crystallized from ethyl acetate to give the title compound, 3.92 g (68.5 %) mp 190-193° C.

1. customThe reaction mixture was evaporated to dryness in vacuo
2. customthe residue evaporated twice with toluene
3. customThe solvents were evaporated in vacuo
4. additionthe residue suspended in a mixture of diethyl ether and 1 M NaOH solution
5. customThe solid was collected
6. customcrystallized from ethyl acetate