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Enantioselective Synthesis of a Dual Orexin Receptor Antagonist

  作者 MANGION IAN K; SHERRY BENJAMIN D; YIN JINGJUN; FLEITZ FRED J  
  选自 期刊  Organic Letters;  卷期  2012年14-13;  页码  3458-3461  
  关联知识点  
 

[摘要]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.

 
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