Palladium-Catalyzed C–H Heteroarylation of 2,5-Disubstituted Imidazoles

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  • Togo Takaya
    Graduate School of Pharmaceutical Sciences, The University of Tokyo
  • Sohma Youhei
    Graduate School of Pharmaceutical Sciences, The University of Tokyo
  • Kuninobu Yoichiro
    Institute for Materials Chemistry and Engineering, Kyushu University
  • Kanai Motomu
    Graduate School of Pharmaceutical Sciences, The University of Tokyo

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  • Communication to the Editor : Palladium-Catalyzed C-H Heteroarylation of 2,5-Disubstituted Imidazoles

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<p>We developed a palladium-catalyzed C–H N-heteroarylation of N-protected-2,5-disubstituted imidazoles at the C4-position using N-heteroaryl halides as a coupling partner. Intensive reaction condition screening led us to identify fluorinated bathophenanthroline 7 as the optimum ligand for the palladium catalyst. This reaction will enhance lead optimization of drug candidates by facilitating the synthesis of heterobiaryl compounds containing an imidazole ring.</p>

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