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Abstract <p>A one-pot telescopic approach has been developed for the safe, scalable, and efficient synthesis of substituted 2-arylimidazo[1,2-<i>a</i>]pyridines starting from commercially available and inexpensive substituted acetophenones and 2-aminopyridine. The procedure involves the in situ formation of phenacyl bromides via chemoselective bromination of acetophenones with <i>N</i>-bromosuccinimide, followed by nucleophilic substitution and heterocyclization with 2-aminopyridine to yield 2-arylimidazo[1,2-<i>a</i>]pyridines. This streamlined telescopic method avoids handling and isolation of hazardous and lachrymatory phenacyl bromides. Moreover, this synthetic protocol eliminates unit operations such as solvent extraction, solvent evaporation/distillation, and final product purification. Notably, the practical utility of this telescopic approach has been demonstrated on a gram scale, affording the product in good yields.</p>

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Efficient, Safe, and Scalable One-Pot Telescopic Synthesis of 2-Arylimidazo[1,2-a]pyridines

  • 期刊论文

  • 发表日期：

    2026年3月1日

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  • S. S. Deshmukh,
  • S. T. Disale,
  • D. H. More,
  • S. S. Pardeshi,
  • B. M. Sapkal

摘要

Abstract

A one-pot telescopic approach has been developed for the safe, scalable, and efficient synthesis of substituted 2-arylimidazo[1,2-a]pyridines starting from commercially available and inexpensive substituted acetophenones and 2-aminopyridine. The procedure involves the in situ formation of phenacyl bromides via chemoselective bromination of acetophenones with N-bromosuccinimide, followed by nucleophilic substitution and heterocyclization with 2-aminopyridine to yield 2-arylimidazo[1,2-a]pyridines. This streamlined telescopic method avoids handling and isolation of hazardous and lachrymatory phenacyl bromides. Moreover, this synthetic protocol eliminates unit operations such as solvent extraction, solvent evaporation/distillation, and final product purification. Notably, the practical utility of this telescopic approach has been demonstrated on a gram scale, affording the product in good yields.