SYNTHESIS OF ARYL ALPHA,ALPHA-DIFLUOROALKYL KETONES AS POTENT INHIBITORS OF CHOLESTEROL ESTERASE

被引:6
|
作者
LIN, GL
LIU, HC
WU, FC
CHEN, SJ
机构
[1] Department of Chemistry, National Chung Using University, Taichung
关键词
ARYL ALPHA; ALPHA-DIFLUOROALKYL KETONE; INHIBITORS OF CHOLESTEROL ESTERASE;
D O I
10.1002/jccs.199400013
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Aryl alpha,alpha-difluoroalkyl ketones were synthesized from the reaction of ethyl alpha,alpha-difluoroacylate with aryl lithium at -78-degrees-C or from the coupling of aryl iododifluoromethyl ketone with 1-alkene in the presence of teterakis(triphenylphosphine)palladium(0). These compounds were potent inhibitors of pancreatic cholesterol esterase with K(i) values in the range 15 muM-20 nM.
引用
收藏
页码:103 / 108
页数:6
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