反应详情

2-Butoxy-8-methoxy-9H-purin-6-amine trifluoroacetate salt (0.2 g) in dry N,N-dimethylformamide (5 mL) was heated at 60° C. with anhydrous potassium carbonate (0.315 g) for 1 hour and allowed to cool to room temperature before adding 3-(bromomethyl)tetrahydro-2H-pyran (0.112 g). The reaction mixture was heated at 50° C., overnight. The reaction mixture was quenched with water (20 mL) and extracted into ethyl acetate (3 times, 75 mL combined volume). The organic phase was separated, combined and passed through a hydrophobic frit to dry. The organic phase was evaporated under reduced pressure to give a yellow oil which was purified by C18 reverse phase chromatography using water (containing 0.1% formic acid)-acetonitrile (containing 0.05% formic acid) as eluant (20-60%) to afford the title compound as a white solid (105.4 mg).

1. temperatureThe reaction mixture was heated at 50° C., overnight
2. customThe reaction mixture was quenched with water (20 mL)
3. extractionextracted into ethyl acetate (3 times, 75 mL combined volume)
4. customThe organic phase was separated
5. customto dry
6. customThe organic phase was evaporated under reduced pressure
7. customto give a yellow oil which
8. customwas purified by C18 reverse phase chromatography