Cesium carbonate → HCID 89699797, compound

Participants

Reaction Steps

Under nitrogen, 2.93 g (10.4 mmol) of the compound of Example 81A together with 2.47 g (11.4 mmol) of 2-bromo-4-nitrotoluene, 233 mg (1.04 mmol) of palladium(II) acetate, 901 mg (1.56 mmol) of xantphos [4,5-bis(diphenylphosphino)-9,9-dimethylxanthene] and 10.2 g (31.1 mmol) of caesium carbonate in 43 ml of 1,4-dioxane were heated under reflux for 3 h. After cooling, the mixture was filtered through Celite, the filter cake was washed with ethyl acetate and the filtrate was concentrated under reduced pressure. The crude product obtained in this manner was purified on a Biotage system (100 g Snap column; mobile phase gradient ethyl acetate/0-8% methanol). This gave 3.26 g (75% of theory) of the title compound.

Provenance & Evidence