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Abstract <p>The primary objective of this study was to develop a sustainable and efficient catalytic method for the synthesis of biologically significant heterocyclic frameworks. Herein we report a simple and green protocol for the one-pot synthesis of 3,4-dihydropyrimidin-2(1<i>H</i>)-ones via the Biginelli cyclocondensation of ethyl acetoacetate, urea, and substituted benzaldehydes using zinc triflate [Zn(OTf)₂] as a Lewis acid catalyst in an aqueous medium. The catalytic performance of Zn(OTf)<sub>2</sub> was comprehensively evaluated by optimizing reaction parameters such as catalyst loading, solvent nature, and temperature. A plausible mechanistic pathway is proposed to elucidate the role of Zn(OTf)<sub>2</sub> in promoting the condensation process. Recyclability studies confirmed the reusability of the Zn(OTf)<sub>2</sub> catalyst with minimal loss of activity. Under the optimized conditions, eleven 3,4-dihydropyrimidin-2(1<i>H</i>)-one derivatives were obtained in high yields (72–94%), demonstrating the efficiency, reproducibility, and green credentials of the developed methodology.</p>

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Green and Recyclable Lewis Acid-Catalyzed Synthesis of 3,4-Dihydropyrimidin-2(1H)-ones in Aqueous Medium

  • 期刊论文

  • 发表日期：

    2026年3月1日

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  • P. R. Pande,
  • A. S. Patki,
  • K. S. Niralwad

摘要

Abstract

The primary objective of this study was to develop a sustainable and efficient catalytic method for the synthesis of biologically significant heterocyclic frameworks. Herein we report a simple and green protocol for the one-pot synthesis of 3,4-dihydropyrimidin-2(1H)-ones via the Biginelli cyclocondensation of ethyl acetoacetate, urea, and substituted benzaldehydes using zinc triflate [Zn(OTf)₂] as a Lewis acid catalyst in an aqueous medium. The catalytic performance of Zn(OTf)2 was comprehensively evaluated by optimizing reaction parameters such as catalyst loading, solvent nature, and temperature. A plausible mechanistic pathway is proposed to elucidate the role of Zn(OTf)2 in promoting the condensation process. Recyclability studies confirmed the reusability of the Zn(OTf)2 catalyst with minimal loss of activity. Under the optimized conditions, eleven 3,4-dihydropyrimidin-2(1H)-one derivatives were obtained in high yields (72–94%), demonstrating the efficiency, reproducibility, and green credentials of the developed methodology.