Cesium carbonate → HCID 68822444, compound

Participants

Reaction Steps

1.0 g (4.13 mmol) of (E)-3-(6-bromopyridin-3-yl)acrylic acid methyl ester, 782.8 mg (4.95 mmol) of 2,4-difluorophenylboronic acid, 108.4 mg (0.413 mmol) of triphenylphosphane, 46.38 mg (0.2 mmol) of palladium(II)acetate and 1.75 g (5.37 mmol) of cesium carbonate were stirred in 40 ml of dioxane and 15 ml water under argon at 100° C. for 6 h. The mixture was filtered, evaporated and the residue dissolved in methanol. By treatment with thionyl chloride the partially saponified methyl ester was re-esterified. After evaporation, the crude product was purified by chromatography (RP18, acetonitrile/water containing 0.1% TFA). Yield: 434 mg (25%).

Provenance & Evidence