Enantioselective Synthesis of a Dual Orexin Receptor Antagonist

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• 作者：Ian K. Mangion ; Benjamin D. Sherry ; Jingjun Yin ; Fred J. Fleitz
• 刊名：Organic Letters
• 出版年：2012
• 出版时间：July 6, 2012
• 年：2012
• 卷：14
• 期：13
• 页码：3458-3461
• 全文大小：257K
• 年卷期：v.14,no.13(July 6, 2012)
• ISSN：1523-7052

文摘

A concise, enantioselective synthesis of the potent dual orexin inhibitor suvorexant (1) is reported. Key features of the synthesis include a mild copper-catalyzed amination, a highly chemoselective conjugate addition, and a tandem enantioselective transamination/seven-membered ring annulation. The synthesis requires inexpensive starting materials and only four linear steps for completion.