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Synthesis of Aryl α,α‐Difluoroalkyl Ketones as Potent Inhibitors of Cholesterol Esterase
Author(s) -
Lin Gialih,
Liu HsiaoChien,
Wu FangChen,
Chen ShowJane
Publication year - 1994
Publication title -
journal of the chinese chemical society
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.329
H-Index - 45
eISSN - 2192-6549
pISSN - 0009-4536
DOI - 10.1002/jccs.199400013
Subject(s) - chemistry , aryl , ketone , triphenylphosphine , alkene , methyl ketone , palladium , lithium (medication) , organic chemistry , catalysis , medicine , alkyl
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.