反应详情

温度

60 °C

To a solution of N2-butyl-8-methoxy-9H-purine-2,6-diamine trifluoroacetic acid salt (3.89 g) in dry N,N-dimethylformamide (46 ml) at room temperature and under was added potassium carbonate (6.14 g) in one go. The reaction was heated to 60° C., under nitrogen, for 1.5 hours. A solution of tetrahydro-3-furanylmethyl methanesulfonate, Isomer 1 (2.2 g) in dry N,N-dimethylformamide (2 ml) was added via a Pasteur pipette and the reaction heated at 70° C. for 16 hours. The reaction was cooled to room temperature, diluted with ethyl acetate (100 ml) and washed with brine (20 ml). The organic layer was concentrated in vacuo. The product was purified by C18 reverse phase chromatography using water (0.1% formic acid)-acetonitrile (0.05% formic acid) as eluant (10-50%) to afford the title compound as a clear viscous oil (2.79 g).

1. temperaturethe reaction heated at 70° C. for 16 hours
2. temperatureThe reaction was cooled to room temperature
3. washwashed with brine (20 ml)
4. concentrationThe organic layer was concentrated in vacuo
5. customThe product was purified by C18 reverse phase chromatography