Cesium carbonate → 4'-[4-[4-(cis-2,6-Dimethylmorpholin-4-yl)phenyl]piperazin-1-yl]-1,1'-biphenyl-4-carboxylic acid methyl ester

Participants

Reaction Conditions

Reaction Steps

To a mixture of cesium carbonate (6.33 q), palladium(II) acetate (156 mg) and 2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (648 mg) in dioxane (28 ml) was successively added cis-2,6-dimethyl-4-(4-piperazinylphenyl)morpholine (4.59 g) and 4′-trifluoromethanesulfonyloxy-1,1′-biphenyl-4-carboxylic acid methyl ester (5 g) in a stream of nitrogen. The mixture was stirred at ambient temperature for 30 minutes and at 80° C. for a further 28 hours. After cooling to room temperature, water was added to the reaction mixture. The resulting precipitates were filtered, washed with water and dried to give 4′-[4-[4-(cis-2,6-dimethylmorpholin-4-yl)phenyl]piperazin-1-yl]-1,1′-biphenyl-4-carboxylic acid methyl ester (3.72 g).

Provenance & Evidence