Synthesis of Aminofuran-Linked Benzimidazoles and Cyanopyrrole-Fused Benzimidazoles by Condition-Based Skeletal Divergence

ACS Comb Sci. 2017 Jul 10;19(7):492-499. doi: 10.1021/acscombsci.7b00052. Epub 2017 May 3.

Abstract

A condition-based skeletal divergent synthesis was explored to achieve skeletal diversity in two component condensation reaction. Cyanomethyl benzimidazole was reacted with α-bromoketone under thermal conditions to furnish 2-aminofuranyl-benzimidazoles, while the same reaction afforded 3-cyano-benzopyrrolo-imidazoles under microwave irradiation. Two nonequivalent nucleophilic centers on benzimidazole moiety were manipulated elegantly by different reaction conditions to achieve the skeletal diversity.

Keywords: 2-aminofuranyl-benzimidazole; 3-cyano-benzopyrrolo-imidazole; divergent synthesis; nonequivalent nucleophilicity; skeletal diversity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzimidazoles / chemical synthesis*
  • Furans / chemical synthesis*
  • Imidazoles / chemical synthesis*
  • Magnetic Resonance Imaging
  • Mass Spectrometry
  • Microwaves
  • Molecular Structure
  • Nitriles / chemical synthesis*
  • Pyrroles / chemical synthesis*
  • Stereoisomerism

Substances

  • Benzimidazoles
  • Furans
  • Imidazoles
  • Nitriles
  • Pyrroles