Elusive Metal-Free Primary Amination of Arylboronic Acids: Synthetic Studies and Mechanism by Density Functional Theory.

Herein, we disclose the first metal-free synthesis of primary aromatic amines from arylboronic acids, a reaction that has eluded synthetic chemists for decades. This remarkable transformation affords structurally diverse primary arylamines in good chemical yields, including a variety of halogenated...

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Publicado en:Journal of the American Chemical Society Vol. 134; no. 44; pp. 18253 - 18257
Autores principales: Chen Zhu, Gongqiang Li, Ess, Daniel H., Falck, John R., Kürti, László
Formato: Artículo
Publicado: American Chemical Society 11/7/2012
Materias:
Acceso en línea:Ver este registro en EBSCOhost
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      dt: 11/7/2012
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      pub: American Chemical Society
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        10.1021/ja309637r
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        atl: Elusive Metal-Free Primary Amination of Arylboronic Acids: Synthetic Studies and Mechanism by Density Functional Theory.
      aug:
        au:
          Chen Zhu
          Gongqiang Li
          Ess, Daniel H.
          Falck, John R.
          Kürti, László
        affil:
          Division of Chemistry, Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, United States
          Department of Chemistry and Biochemistry, Brigham Young University, Provo, Utah 84602, United States
      su:
        Amination
        Boronic acids
        Density functionals
        Aromatic amines
        Organic compounds
      sug:
        subj:
          Amination
          Boronic acids
          Density functionals
          Aromatic amines
          Organic compounds
      ab: Herein, we disclose the first metal-free synthesis of primary aromatic amines from arylboronic acids, a reaction that has eluded synthetic chemists for decades. This remarkable transformation affords structurally diverse primary arylamines in good chemical yields, including a variety of halogenated primary anilines that often cannot be prepared via transition-metal-catalyzed amination. The reaction is operationally simple, requires only a slight excess of aminating agent, proceeds under neutral or basic conditions, and, importantly, can be scaled up to provide multigram quantities of primary anilines. Density functional calculations reveal that the most likely mechanism involves a facile 1,2-aryl migration and that the presence of an ortho nitro group in the aminating agent plays a critical role in lowering the free energy barrier of the 1,2-aryl migration step.
      pubtype: Academic Journal
      doctype: Article
      src: R
    language: English
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