3′R,4′R-二取代角型吡喃香豆素的不对称合成(英文)  

Total Asymmetric Synthesis of 3′R,4′R-Disubstituted Angular Dihydropyranocoumarins

作　　者：孙视[1] 孔令义[1] 张涵庆[2] 贺善安[2] 

机构地区：[1]中国药科大学天然药物化学教研室,南京210038 [2]中国科学院植物研究所,南京210014

出　　处：《中国药科大学学报》2005年第3期205-209,共5页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.29872058);高等学校优秀青年教师科研奖励计划资助项目~~

摘　　要：目的:寻找具有钙离子拮抗作用和乙酰胆碱酯酶抑制活性双重作用机制的早老性痴呆(Alzheimer′sDisease,AD)新型抑制剂。方法:间二苯酚为底物,AD-mix-β作不对称双羟基化试剂进行凯林内酯类香豆素的全合成;所有产物进行乙酰胆碱酯酶(AchE)抑制活性测试。结论:立体选择性地合成cis3′-R,4′R-二取代角型二氢吡喃香豆素,但AchE抑制活性明显低于cis3′-R,4′R-二取代线型二氢吡喃香豆素。AIM:To obtain new typical compounds with dual mechanism,antagonizing Ca^(2+)and inhibiting acetylcholinesterase,on Alzheimer's disease.METHODS:Resorcinol was chosen as primitive substrate,and AD-mix-β as asymmetrically dihydroxylated reagent;all products were screened against acetylcholinesterase in vitro.RESULTS:cis-3′R,4′R-disubstituted angular dihydropyranocoumarins were synthesized enantioselectively,however,its inhibitory activity on acetylcholinesterase is distinctively lower than that of cis-3′R,4′R-disubstituted linear dihydropyranocoumarins.

关 键 词：3′R 4′R-凯林内酯类香豆素 不对称双羟基化 早老性痴呆 乙酰胆碱酯酶抑制剂 钙离子拮抗剂 

分 类 号：TQ460.1[化学工程—制药化工]