Citation: Jian Jun Xue, Xiao Ming Yu. Selective 3- and 6-OH modification of (-)-clausenamide[J]. Chinese Chemical Letters, ;2011, 22(7): 671-764. doi: 10.1016/j.cclet.2011.01.026 shu

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

Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China

Received Date: 29 November 2010

Fund Project: This project was financially supported by Natural Science Foundation of China (No.30672530).

(-)-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 3-0-methyl, 6-0-methyl, 3-des-hydroxyl and 6-des-hydroxyl analogues were prepared by selective 3- and 6- OH modification of (-)-clausenamide.
- (-)-Clausenamide,
- Derivatives,
- Synthesis,
- Alzheimer's diseas
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