Selective 3-and 6-OH modification of (-)-clausenamide  

作　　者：Jian Jun Xue Xiao Ming Yu 

机构地区：[1]Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China

出　　处：《Chinese Chemical Letters》2011年第7期761-764,共4页中国化学快报（英文版）

基　　金：financially supported by Natural Science Foundation of China(No.30672530)

摘　　要：（-）-Clausenamide is a drug candidate under Phase I clinical trial for treatment of Alzheimer＇s disease （AD）. In order to elucidate the substituent related structure-activity relationship, six one-substituent modified （-）-clausenamide analogues were designed, and four of them, namely 3-O-methyl, 6-O-methyl, 3-des-hydroxyl and 6-des-hydroxyl analogues were prepared by selective 3- and 6- OH modification of （-）-clausenamide.（-）-Clausenamide is a drug candidate under Phase I clinical trial for treatment of Alzheimer＇s disease （AD）. In order to elucidate the substituent related structure-activity relationship, six one-substituent modified （-）-clausenamide analogues were designed, and four of them, namely 3-O-methyl, 6-O-methyl, 3-des-hydroxyl and 6-des-hydroxyl analogues were prepared by selective 3- and 6- OH modification of （-）-clausenamide.

关 键 词：（-）-Clausenamide DERIVATIVES SYNTHESIS Alzheimer＇s disease 

分 类 号：TQ463.4[化学工程—制药化工] S816.15[农业科学—饲料科学]