Cesium carbonate → HCID 66980978, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 4-bromo-2-(trifluoromethyl)benzonitrile (0.1 g, 0.4 mmol) dissolved in 1,4-Dioxane (5 mL), (R)-benzyl 1-methyl-2-oxoimidazolidine-4-carboxylate (25c) (0.093 g, 0.4 mmol) was added at room temperature followed by Cs2CO3 (0.260 g, 0.8 mmol) and Argon gas was purged for 30 min. To the reaction mixture Pd2(dba)3 (0.036 g, 0.04 mmol) and Xanthphos (0.034 g, 0.058 mmol) were added at room temperature. The resulting reaction mixture was then heated to 100° C. for 5 h. After completion (by TLC), the reaction mixture was filtered through celite bed. The celite bed was washed with EtOAc (2×5 mL), the filtrates were combined, dried over Na2SO4 and concentrated under reduced pressure to give the crude compound. The crude residue was purified by column chromatography to provide 25d (0.075 g, 46%) as a colourless syrup.

Provenance & Evidence