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Selective 3-and 6-OH modification of (-)-clausenamide 被引量：4

Selective 3-and 6-OH modification of (-)-clausenamide
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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.
作者 Jian Jun Xue Xiao Ming Yu
机构地区 Institute of Materia Medica
出处 《Chinese Chemical Letters》 SCIE CAS CSCD 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)
关键词 （-）-Clausenamide DERIVATIVES SYNTHESIS Alzheimer＇s disease （-）-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]
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  • 10Analytical data for compounds 2-5. Compound 2: mp: 191.0-191.9 C; [a]20 -184.3 (c 1.07, CHC13); 1H NMR (300 MHz, CDCI3): 2.84 (s,3H), 3.55 (s, 3H), 3.83 (d, 1H, J = 9.0 Hz), 3.81 (dd, 1H, J = 9.0, 8.7 Hz), 4.i5 (dd, 1H, J = 4.2, 8.7 Hz), 4.75 (d, 1H, J = 4.2 Hz), 6.85-7.37 (m,10H).

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Chinese Chemical Letters
2011年 第7期

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