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甲基苯磺酰胺类CCR5生物拮抗剂的合成及表征 被引量:1

Synthesis and Structural Characterization of Methylbenzenesulfonamide CCR5 Antagonists
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摘要 以1-苯甲基-4-哌啶酮合成了4-甲基-N-乙基-N-(4-哌啶基)苯磺酰胺(中间体7),以4-氯苯甲氯为原料,通过溴化及还原合成了5-溴-2-(4-氯苯甲氧基)溴甲基苯(中间体3),通过中间体7和中间体3合成了一种新的小分子化合物4-甲基-N-乙基-N-(N-(5-溴-2-(4-氯苯甲基氧基)苯甲基)-4-哌啶基)苯磺酰胺,对该产物进行了1 H NMR、MS、IR表征及生物活性检测,结果表明该化合物可以作为药物开发的候选化合物. Interest in the methylbenzenesulfonamide has been increasing due to pyridine,benzenesulfo-nyl,bromine atom such as active group.The small molecular antagonists can be used as a targeting prepa-ration in the prevention of human HIV-1 infection.4-methyl-N-ethyl-N-(piperidin-4-yl)benzenesulfon-amide(intermediate 7 )was prepared from N-Benzyl-4-piperidone.4-bromo-1-((4-chlorobenzyl)oxy)-2-(bromomethyl)benzene(intermediate 3)was synthesized from 1-chloro-4-(chloromethyl)benzene.Further reaction of 7 with 3 gave a novel compound 4-methyl-N-(1-(5-bromo-2-((4-chlorobenzyl)oxy)benzyl)piper-idin-4-yl)-N-ethylbenzenesulfonamide.The compounds were characterized by 1 H NMR,MS,IR and bioac-tivity.The compound can be used as the candidate compounds for drug development.
出处 《内蒙古师范大学学报(自然科学汉文版)》 CAS 北大核心 2015年第4期477-480,共4页 Journal of Inner Mongolia Normal University(Natural Science Edition)
基金 国家自然科学基金资助项目(51303115) 四川省教育厅资助项目(15ZB0215) 自贡市重点科技计划项目(2014ZC01)
关键词 苯磺酰胺 非肽类小分子化合物 生物拮抗剂 1-苯甲基-4-哌啶酮 4-氯苯甲氯 benzenesulfonamide non-peptide small molecular compounds biological antagonists N-Benzyl-4-piperidone 1-chloro-4-(chloromethyl)benzene
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参考文献10

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二级参考文献22

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