抗胆碱药2-(1-萘基)-2-环戊基-2-羟基乙氧基环烃胺类化合物的合成  

Synthesis of Anticholinergics of 2(1Naphthyl)2Cyclopentyl2Hydroxy Ethoxy Cyclic Amine Compounds

作　　者：吴培金[1] 恽榴红[1] 

机构地区：[1]军事医学科学院毒物药物研究所

出　　处：《中国药物化学杂志》1999年第2期102-105,共4页Chinese Journal of Medicinal Chemistry

摘　　要：设计合成了３个三取代乙氧基环烃胺类新化合物和２个未知中间体．药理实验表明：化合物（Ⅱ１）有较好的抗胆碱作用，化合物（Ⅱ２），（Ⅱ３）作用不明显；表明以萘基替代苯基，抗胆碱作用降低．These compounds were synthesized by four steps.1)1Naphthonitrile()was prepared by reacting 1bromonaphthalene with cuprous cyanide.2)The 1naphthyl cyclopentyl ketone()was obtained by the Grignard reaction.3)Through the Wittig reaction,the ketone ()was transformed to relative oxirane().4)The final products(1)(3)were obtained by reacting oxirane()with 3quinuclidinol,Nmethyl4piperidnol and 3tropanol respectively.Five new compounds,including the intermediates(),()and the end products(1)(3)were not yet reported in literature.The preliminary anticholinergic activities of these compounds were tested in mice and the results showed compound(1)had moderate activity.

关 键 词：抗胆碱药物 维悌希反应 乙氧基环烃胺 合成 

分 类 号：TQ463.3[化学工程—制药化工]