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【结 构 式】 
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【药物名称】 【化学名称】6-O-Demethyl-6-O-(N-methylcarbamoyl)galanthamine 【CA登记号】 【 分 子 式 】C18H22N2O4 【 分 子 量 】330.38704 |
【开发单位】Aventis Pharma (Originator) 【药理作用】Cognition Disorders, Treatment of, NEUROLOGIC DRUGS, Acetylcholinesterase Inhibitors |
合成路线1
The demethylation of galanthamine (I) with ethyl mercaptane sodium salt in hot DMF gives 6-demethylgalanthamine (II), which is selectively monoesterified at the phenolic OH with N-methylcarbamic acid and CDI yielding the target monoester. The selective monoesterification of (II) can also be performed with N-methylcarbamic anhydride and TEA or DMAP, with N-methylcarbamoyl chloride and DBU, with N-methylisocyanate and K2CO3 or with CDI and methylamine in HOAc.
| 【1】 Bores, G.M.; Kosley, R.W. Jr.; Galanthamine derivatives for the treatment of Alzeimer's disease. Drugs Fut 1996, 21, 6, 621. |