Regioselective synthesis of benzimidazole thiophene inhibitors of polo-like kinase 1

Keith R. Hornberger, Jennifer G. Badiang, James M. Salovich, Kevin W. Kuntz, Kyle Allen Emmitte, Mui Cheung

Research output: Contribution to journalArticlepeer-review

23 Scopus citations

Abstract

A regioselective synthesis of novel 1-(2-thienyl)-benzimidazole inhibitors of polo-like kinase 1 is described. Amination of substituted 2-iodo or -bromo nitrobenzenes with a 2-aminothiophene derivative catalyzed by Pd2dba3 and XANTPHOS in the presence of excess Cs2CO3 afforded good yields of the coupled products. Subsequent reduction and cyclization of these intermediates provided the desired benzimidazole compounds.

Original languageEnglish
Pages (from-to)6348-6351
Number of pages4
JournalTetrahedron Letters
Volume49
Issue number44
DOIs
StatePublished - 27 Oct 2008

Keywords

  • Amination
  • Benzimidazoles
  • Catalysis
  • PLK
  • Palladium-catalyzed

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