4.7 Article

Copper-Catalyzed Synthesis of 2-Unsubstituted, N-Substituted Benzimidazoles

Journal

JOURNAL OF ORGANIC CHEMISTRY
Volume 74, Issue 24, Pages 9570-9572

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/jo902160y

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Funding

  1. Deutsche Forschungsgemeinschaft
  2. Fonds der Chemischen Industrie
  3. Deutsche Akademische Austauschdienst
  4. Alexander von Humboldt Foundation
  5. Young University Teachers of the Alfried Krupp von Bohlen und Halbach Foundation

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An efficient copper-catalyzed intramolecular arylation of formamidines forming 2-unsubstituted benzimidazoles in excellent yields is reported. Sixteen examples bearing sterically demanding substituents on nitrogen like Mes, 2,6-diisopropylphenyl, or 2-tert-butylphenyl and tolerating various functional groups demonstrate the utility of this method.

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