An Efficient One-pot Conversion of Carboxylic Acids into Benzimidazoles an HBTU-promoted Methodology

Overview

Journal RSC Adv

Publisher Royal Society of Chemistry

Specialty Chemistry

Date 2022 May 13

PMID 35547918

Authors

Leonard Barasa

Sabesan Yoganathan

Affiliations

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Abstract

Benzimidazole is a privileged, and routinely used pharmacophore in the drug discovery process. Herein, we report a mild, acid-free and one-pot synthesis of indole, alkyl and alpha-amino benzimidazoles through a novel HBTU-promoted methodology. An extensive library of indole-carboxylic acids, alkyl carboxylic acids and -protected alpha-amino acids has been converted into the corresponding benzimidazoles in 80-99% yield. Since alpha-aminobenzimidazoles are highly useful synthons as chiral ligands for chemical catalysis, as well as for drug discovery endeavors, our reported method provides direct access to this scaffold in a simple, one-pot operation from commercially available carboxylic acids.

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