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 Ki values in the range 15 μM‐20 nM.
Lipase from porcine pancreas was demonstrated to catalyze reactions under azeotropic and ultrasonic conditions. Reaction rates were significantly enhanced 3 to 60‐fold by applying azeotropic distillation and 7 to 83‐fold by applying ultrasonication. For both conditions, enantioselectivities were retained.
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