Synthesis of (鈭?-Homogalanthamine from Naltrexone

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• 作者：Naoshi Yamamoto ; Hideaki Fujii ; Satomi Imaide ; Shigeto Hirayama ; Toru Nemoto ; Junji Inokoshi ; Hiroshi Tomoda ; Hiroshi Nagase
• 刊名：Journal of Organic Chemistry
• 出版年：2011
• 出版时间：April 1, 2011
• 年：2011
• 卷：76
• 期：7
• 页码：2257-2260
• 全文大小：825K
• 年卷期：v.76,no.7(April 1, 2011)
• ISSN：1520-6904

文摘

Acetylcholinesterase inhibitor (鈭?-homogalanthamine 3 was synthesized from 渭 opioid antagonist naltrexone (2) in 16% total yield. The synthesis features Grob fragmentation as a key reaction, which was especially accelerated in the presence of 15-crown-5.