4.8 Article

Copper-catalyzed regiospecific synthesis of N-alkylbenzimidazoles

Journal

ORGANIC LETTERS
Volume 9, Issue 23, Pages 4749-4751

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol7020737

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Funding

  1. NCI NIH HHS [CA 09112] Funding Source: Medline
  2. NIGMS NIH HHS [GM 58160, F32 GM 074407] Funding Source: Medline

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A copper-catalyzed method is described for the preparation of N-alkylbenzimidazoles in regioisomerically pure form starting from o-haloanilines. The method utilizing CuI and trans-N,N'-dimethyl-1,2-cyclohexanediamine allows the preparation of N-alkylbenzimidazoles in good to excellent yields.

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