西北师范大学学报（自然科学版）Issue(4)：58-61,85,5.
4-甲基-N-烯丙基-N-（1-（5-溴-2-（对氯苄基氧基）苄基）-4-哌啶基）苯磺酰胺的合成及生物活性研究
Synthesis and biological activities of N-allyl-N-(1-(5-bromo-2-((4-chlorobenzyl)oxy)benzyl) piperidin-4-yl)-4-methylbenzenesulfonamide
摘要
Abstract
4‐Bromo‐2‐(bromomethyl )‐1‐((4‐chlorobenzyl ) oxy ) benzene (intermediate 3 ) is synthesized from 1‐chloro‐4‐(chloromethyl ) benzene and 5‐bromo‐2‐hydroxybenzaldehyde by elimination reaction , reduction reaction and bromization in turn . N‐allyl‐4‐methyl‐N‐( piperidin‐4‐yl ) benzenesulfonamide (intermediate 7 ) is prepared from 1‐benzylpiperidin‐4‐one . Further reaction of intermediate 3 with intermediate 7 can give a novel non‐peptide CCR5 antagonist N‐allyl‐N‐(1‐(5‐bromo‐2‐((4‐chlorobenzyl ) oxy)benzyl)piperidin‐4‐yl)‐4‐methyl benzenesulfonamide .The compounds are characterized by 1 HNMR , 13CNMR ,IR , MS .The biological activity of the antagonist is detected . The results show that the antagonist is the target peoduct with good biological activity and the total yield is about 26% .关键词
CCR5拮抗剂/苯磺酰胺/非肽类小分子化合物/生物活性Key words
CCR5 antagonist/benzenesulfonamide/non-peptide small molecular compounds/bioactivity分类
化学化工引用本文复制引用
黄斌,程德军,李明田..4-甲基-N-烯丙基-N-（1-（5-溴-2-（对氯苄基氧基）苄基）-4-哌啶基）苯磺酰胺的合成及生物活性研究[J].西北师范大学学报（自然科学版）,2015,(4):58-61,85,5.基金项目
四川省教育厅基金资助项目（15ZB0215）；自贡市重点科技计划项目 （）
