环状胺磺酰基取代的苯乙胺和苯氧烷胺衍生物的合成及生物活性测试  

Synthesis and Biological Activity of Cyclosulfamido Substituted Phenylethylamine and Phenoxylalkylamine Derivatives

作　　者：习保民[1] 江振洲[2] 王涛[2] 倪沛洲[3] 

机构地区：[1]南方医科大学药学院药物化学系,广州510515 [2]中国药科大学新药筛选中心,南京210038 [3]中国药科大学有机化学教研室,南京210038

出　　处：《有机化学》2009年第7期1161-1164,共4页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.30600776);863计划(No.2002AA2Z3118)资助项目

摘　　要：7-氨基乙基-(3,4-二氢-2H-苯并[1,2]噻嗪-1,1-二氧代)盐酸盐和取代苯氧丙-2-酮经还原胺化,合成了10个新的环状胺磺酰基取代的苯乙胺和苯氧烷胺类化合物.化合物经1HNMR,HRMS,IR确证其结构.生物活性测试结果表明,所有化合物对α1-肾上腺素受体均具有一定的拮抗作用。A series of novel cyclosulfamido substituted phenoxylalkylamine derivatives were synthesized through the condensation and reduction of various substituted phenoxypropan-2-one with 7-（2-aminoethyl- 3,4-dihydro- 1,1-dioxo-2H-benzo[e][1,2]thiazine）laydrocholoride （5）. Their structures were identified by ^1H NMR, HRMS, and IR data. The target compounds have been assayed with function analysis in anococcyeus muscle, indicating that all of them have good blocking activity to α1-adrenoceptor.

关 键 词：磺酰胺 合成 α1-肾上腺素受体拮抗剂 

分 类 号：O621.29[理学—有机化学]