甲基苯磺酰胺类CCR5生物拮抗剂的合成及表征  

Synthesis and Structural Characterization of Methylbenzenesulfonamide CCR5 Antagonists

作　　者：程德军[1] 黄斌[1] 李明田[1] 

机构地区：[1]四川理工学院材料与化学工程学院,四川自贡643000

出　　处：《内蒙古师范大学学报（自然科学汉文版）》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)

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.

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 

分 类 号：O623.8[理学—有机化学]