Synthesis of Aryl α,α‐Difluoroalkyl Ketones as Potent Inhibitors of Cholesterol Esterase

Aryl α,α‐difluoroalkyl ketones were synthesized from the reaction of ethyl α,α‐difluoroacylate with aryl lithium at −78°C or from the coupling of aryl iododifluoromethyl ketone with 1‐alkene in the presence of tetcrakis(triphenylphosphine)palladium(0). These compounds were potent inhibitors of pancreatic cholesterol esterase with K i values in the range 15 μM‐20 nM.