反应详情

温度

90 °C

A mixture of 8a (49 mg, 0.15 mmol), cesium carbonate (0.11 g, 2 eq), 5-Methanesulfonyl-2,3-dihydro-1H-indole (35 mg, 1.2 eq), tris(dibenzylideneacetone)-dipalladium (31 mg, 0.1 eq), tri-t-butylphosphonium tetrafluoroborate (37 mg, 0.8 eq) and dioxane (1.5 mL) was heated at 90° C. for 4 h. The mixture cooled to room temperature, dioxane was added and the mixture was filtered and washed with DCM. The filtrate was concentrated under a stream of nitrogen and the residue was taken up in 1 mL of THF and was purified by preparative HPLC to afford 8-1; LCMS 491.2 (MH+), tR=5.35 (Method 6). EC50: 201 nM.

1. temperatureThe mixture cooled to room temperature
2. filtrationthe mixture was filtered
3. washwashed with DCM
4. concentrationThe filtrate was concentrated under a stream of nitrogen
5. customwas purified by preparative HPLC
6. customto afford 8-1