Triazole‐Based Anion‐Binding Catalysis for the Enantioselective Dearomatization of <i>N</i>‐Heteroarenes with Phosphorus Nucleophiles

  • Theresa Fischer
    Institute for Organic Chemistry University of Regensburg Universitätsstr. 31 93053 Regensburg Germany
  • Qui‐Nhi Duong
    Institute for Organic Chemistry University of Regensburg Universitätsstr. 31 93053 Regensburg Germany
  • Olga García Mancheño
    Institute for Organic Chemistry University of Regensburg Universitätsstr. 31 93053 Regensburg Germany

書誌事項

公開日
2017-02-16
権利情報
  • http://onlinelibrary.wiley.com/termsAndConditions#vor
DOI
  • 10.1002/chem.201605660
公開者
Wiley

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説明

<jats:title>Abstract</jats:title><jats:p>The first enantioselective synthesis of chiral heterocyclic α‐amino phosphonates by nucleophilic dearomatization of quinolines and pyridines using an anion‐binding organocatalysis approach is described. Chiral tetrakistriazoles were employed as efficient hydrogen‐bond donor catalysts by forming a chiral close ion‐pair with the in situ formed <jats:italic>N</jats:italic>‐acyl salts and 2,2,2‐trichlorethoxycarbonyl chloride (TrocCl). The ion‐pair was subsequently treated with various phosphorus nucleophiles, such as silyl‐protected dialkyl‐ and trialkylphosphites. Thus, the corresponding products were obtained in complete or high regioselectivities and up to 97:3 e.r. for quinolines or up to 89:11 e.r. for the more challenging pyridine substrates. This method allows for rapid access to substituted chiral cyclic α‐amino phosphonates, which can be easily transformed into phosphonic acid derivatives.</jats:p>

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