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

Article abstract of DOI:10.1016/j.cclet.2011.01.026

(-)-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.