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April 22, 2026The Journal of Organic Chemistry0 citations

Metal-Free Direct Amidation of Nitroarenes with Carboxylic Acids

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AAAkshay M. AkhadeKHKishor L. Handore

Key Points

  • The aim is to develop a simple, metal-free method for the amidation of nitroarenes using carboxylic acids.
  • Utilized in situ activation of carboxylic acids for amidation
  • Performed nitro to amine reduction as part of the process
  • Executed C-N coupling to form amide bonds.
  • Achieved high yields of desired amides
  • Showed broad functional group tolerance
  • Efficiently synthesized important amide scaffolds for pharmaceuticals and agrochemicals.

Abstract

We report a facile, metal-free protocol for the direct amidation of readily available nitroarenes and carboxylic acids. The method proceeds via in situ activation of carboxylic acids, nitro-to-amine reduction, and subsequent C-N coupling to furnish the corresponding amide bond. This transformation exhibits broad functional group tolerance and delivers the desired amides in high yields. The method's applicability is showcased through the efficient synthesis of pharmaceutically and agrochemically important amide scaffolds and rapid derivatization of drug molecules containing carboxylic acid groups.

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Cite This Study

Akhade et al. (2026) studied this question.

synapsesocial.com/papers/69e864866e0dea528dde956chttps://doi.org/10.1021/acs.joc.6c00299
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