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Direct Synthesis of Chiral 1,2,3,4-Tetrahydropyrrolo[1,2-a]pyrazines via a Catalytic Asymmetric Intramolecular Aza-Friedel-Crafts Reaction

  作者 HE YUWEI; LIN MAOHUI; LI ZHONGMIN; LIANG XINTING; LI GUILONG; ANTILLA JON C  
  选自 期刊  Organic Letters;  卷期  2011年13-17;  页码  4490-4493  
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[摘要]The direct asymmetric intramolecular aza-Friedel-Crafts reaction of N-aminoethylpyrroles with aldehydes catalyzed by a chiral phosphoric acid represents the first efficient method for the preparation of medicinally interesting chiral 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazines with high yields and high enantioselectivities. This strategy has been shown to be quite general toward various aldehydes and pyrrole derivatives.

 
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