Liquid-phase synthesis of 2-(alkylthio) benzimidazoles

  • Yeh C
  • Sun C
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An efficient liquid-phase synthesis of 2-alkylthio-5-carbamoylbenzimidazoles 1 is described. Immobilized o-fluoronitrobenzene 2 undergoes nucleophilic addition of primary amine to afford o-nitroaniline derivatives 3. Subsequent reduction of the aromatic nitro group followed by cyclization gives a PEG-bound benzimidazole-2-thione 5. S-Alkylation of polymer-supported scaffold 5 followed by cleavage gives the resulting library in high yield and high purity.

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  • Chih Ming Yeh

  • Chung Ming Sun

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