Two-step solution-phase synthesis of novel benzimidazoles utilizing a UDC (Ugi/de-Boc/cyclize) strategy

Paul Tempest, Vu Ma, Samuel Thomas, Zheng Hua, Michael G. Kelly, Christopher Hulme

Research output: Contribution to journalArticlepeer-review

97 Scopus citations


The novel solution-phase synthesis of an array of biologically relevant benzimidazoles in a simple two-step procedure is revealed. Transformations are carried out in excellent yield by condensation of mono-Boc protected ortho-phenylene diamine and supporting Ugi reagents. Subsequent acid treatment and evaporation affords benzimidazoles in good to excellent yield. The described protocol represents a highly attractive solution-phase procedure for the rapid generation of benzimidazole libraries.

Original languageEnglish (US)
Pages (from-to)4959-4962
Number of pages4
JournalTetrahedron Letters
Issue number30
StatePublished - Jul 23 2001

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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