Cheng De-ju
2015
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Journal
Journal of University of Jinan
Abstract
The 4-bromo-2-( bromomethyl)-1-(( 4-chlorobenzyl) oxy) benzene( intermediate Ⅲ) was synthesized from 1-chloro-4-( chloromethyl) benzene and 5-bromo-2-hydroxybenzaldehyde by elimination reaction,reduction reaction and bromization. N-allyl-2-chloro-N-( piperidin-4-yl) benzamide was prepared from 1-benzylpiperidin-4-one. Further reaction of intermediate Ⅲ with intermediate Ⅶgave a novel non-peptide CCR5 antagonist N-allyl-N-( 1-( 5-bromo-2-(( 4-chlorobenzyl) oxy) benzyl) piperidin-4-yl)-2-chlorobenzamide. By detecting the activity of GTPγS,the hemi-inhibitory concentration( IC50) was( 5. 35 ± 0. 3) nmol/L. The products exhibit certain bioactivities. In addition,the compounds are characterized by1 H NMR,13 C NMR,IR and MS.