【药物名称】AP-2238
化学结构式(Chemical Structure):
参考文献No.727839
标题:3-(4-{[Benzyl(methyl)amino]methyl}phenyl)-6,7-dimethoxy-2H-2-chromenone (AP2238) inhibits both acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation: A dual function lead for Alzheimer's disease therapy
作者:Piazzi, L.; Rampa, A.; Bisi, A.; Gobbi, S.; Belluti, F.; Cavalli, A.; Bartolini, M..; Andrisano, V.; Valenti, P.; Recanatini, M.
来源:J Med Chem 2003,46(12),2279
合成路线图解说明:

Partial demethylation of 2,4,5-trimethoxybenzaldehyde (I) with BCl3 gives 2-hydroxy-4,5-dimethoxybenzaldehyde (II), which is condensed with the sodium salt of p-tolylacetic acid (III) in boiling acetic anhydride to afford the coumarin derivative (IV). Benzylic halogenation of (IV) with N-bromosuccinimide in the presence of a catalytic amount of benzoyl peroxide yields bromide (V), which is finally condensed with N-methyl benzylamine (VI) to afford the desired compound.

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