反应详情

温度

100 °C

55b (30 mg, 0.068 mmol), trimethylboroxine (25 mg, 0.2 mmol) and potassium carbonate (50 mg, 0.36 mmol) were combined in 0.5 mL of dioxane and heated at 100° C. for 20 h. The mixture was cooled, concentrated under a stream of nitrogen, diluted with water (2 mL) and extracted with ethyl acetate (2×2 mL). The combined extracts were dried under a stream of nitrogen and the residue was purified by preparative HPLC to afford 55-1 as a colorless oil: LC-MS 423.1 (MH+), tR=5.95 (Method 2). EC50: 206 nM.

1. temperatureThe mixture was cooled
2. concentrationconcentrated under a stream of nitrogen
3. additiondiluted with water (2 mL)
4. extractionextracted with ethyl acetate (2×2 mL)
5. customThe combined extracts were dried under a stream of nitrogen
6. customthe residue was purified by preparative HPLC