反应详情

温度

80 °C

9-{(3aR,4R,6S,6aR)-6-[3-(tert-butyl)-1,2,4-oxadiazol-5-yl]-2,2-dimethyltetrahydrofuro[3,4-d][1,3]dioxol-4-yl}-6-(1H-1,2,3-benzotriazol-1-yloxy)-9H-purine (50 mg) was dissolved in 2,4-difluoroaniline (0.4 ml) and the mixture heated at 80° C. for 96 h. The mixture was then cooled to 20° C. and partitioned between dichloromethane (25 ml) and 1 M hydrochloric acid (15 ml). The separated aqueous phase was further extracted with dichloromethane (1×25 ml) and the combined organic extracts were evaporated to dryness in vacuo. Purification by automated preparative HPLC afforded the title compound (18.3 mg) as a dark purple gum.

1. temperatureThe mixture was then cooled to 20° C.
2. custompartitioned between dichloromethane (25 ml) and 1 M hydrochloric acid (15 ml)
3. extractionThe separated aqueous phase was further extracted with dichloromethane (1×25 ml)
4. customthe combined organic extracts were evaporated to dryness in vacuo
5. customPurification by automated preparative HPLC