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A Concise Synthesis of 6-Oxa-3-azabicyclo[3.1.1]heptane Hydrotosylate

  作者 WISHKA DONN G; BEAGLEY PAUL; LYON JESSICA; FARLEY KATHLEEN A; WALKER DANIEL P  
  选自 期刊  Synthesis;  卷期  2011年-16;  页码  2619-2624  
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[摘要]Bridged bicyclic morpholines are important building blocks in medicinal chemistry research. The bicyclic morpholine 6-oxa-3-azabicyclo[3.1.1]heptane (2a) is of particular interest as a morpholine isostere because it is achiral and shows properties similar to that of morpholine based on a derived analogue. The first synthesis of morpholine 2a (tosylate salt) is described. The six-step sequence begins with inexpensive starting materials and uses straightforward chemistry.

 
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