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Synthesis of 5-Azaindoles via a Cycloaddition Reaction between Nitriles and Donor-Acceptor Cyclopropanes

  作者 MOUSTAFA MAHMOUD M ABD RABO; PAGENKOPF BRIAN L  
  选自 期刊  Organic Letters;  卷期  2010年12-14;  页码  3168-3171  
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[摘要]A new method for the synthesis of 5-azaindole derivatives is reported. A [3+2] dipolar cycloaddition between nitriles and a 3,4-cyclopropanopiperidirie followed by SeO2 oxidation affords the target compounds in moderate to excellent yields. The divergent nature and cost effectiveness of this method makes it very suitable for combinatorial applications in the pharmaceutical industry.

 
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