Water → 2-(4-tert-Butylphenyl)-4-pyridinyl 4,4,4-trifluoro-1-butanesulfonate

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Reaction Steps

42.2 mg (0.24 mmol) of 4-tert-butylbenzeneboronic acid, 90 mg (0.22 mmol) of 2-trifluoromethylsulfonyloxy-4-pyridinyl 4,4,4-trifluoro-1-butanesulfonate (Example 40A), 12.5 mg (0.01 mmol) of tetrakisphenylpalladium(0) and 68.6 mg (0.65 mmol) of sodium carbonate are heated in 5 ml of dioxane at 80° C. under argon for 2 hours. The reaction mixture is cooled, mixed with 0.5 ml of water and filtered through a cartridge packed with 3 g of Extrelut NT3 (Merck) and thoroughly washed with dichloromethane, and the solvent is distilled off under reduced pressure. The residue is purified by preparative HPLC and chromatography on silica gel (toluene).

Provenance & Evidence