A convenient one-pot synthesis of 2-substituted benzimidazoles

Good Synthesis procedure

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Summary:

An efficient and green method for synthesis of 2 substituted benzimidazoles has been described. Despite previous methods being available in literature for synthesis of such compounds, the ease of operation, use of common and non-toxic solvent and cheap catalyst (NH4Cl) are the highlights of this new methodology.

The general procedure involves the reaction of o-phenylene diamine with a range of substituted aldehydes in the ratio 1:2 in ethanolic medium and in presence of NH4Cl to afford. The procedure is depicted in scheme 1 and the results summarized in Table 1.

Practical observations:

  • The method is very easily reproducible. The reaction times were found to be around 3 hours for most of the reactions.
  • As noted by the authors in the section “Results and Discussion”, the results replicated the observation that the aliphatic aldehydes did not yield more than 10% while the aryl ketones did not react with diamine.

Comments:

  • The novelty of this method is the selective formation of 2 substituted benzimidazoles only without the formation of 1,2 disubstituted ones as side products.
  • The catalyst used is one of the cheapest chemicals available in labs.


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