Synthesis 2025; 57(07): 1329-1338
DOI: 10.1055/a-2508-9681
paper

A Solvent-Free 2-Chloro-1-methylpyridinium Iodide (CMPI)-Mediated Biginelli Reaction for the Construction of 3,4-Dihydropyrimidin-2(1H)-ones/thiones

Authors

  • Ashish Kumar

    a   School of Basic Sciences, Department of Chemistry, Babu Banarasi Das University, Lucknow, Uttar Pradesh 226028, India
    b   Chemistry Innovation Research Center, Jubilant Biosys Ltd, Greater Noida, Uttar Pradesh 201310, India
  • Shashi Pandey

    c   Department of Chemistry, Faculty of Science, University of Lucknow, Lucknow, Uttar Pradesh 226007, India
  • Monika Gupta

    a   School of Basic Sciences, Department of Chemistry, Babu Banarasi Das University, Lucknow, Uttar Pradesh 226028, India
  • Chatrasal S. Rajput

    b   Chemistry Innovation Research Center, Jubilant Biosys Ltd, Greater Noida, Uttar Pradesh 201310, India


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Abstract

The Biginelli product dihydropyrimidinones (DHPMs) and their derivatives have enormous biological significance. This article describes the exploration of 2-chloro-1-methylpyridinium iodide (CMPI) reagent for the development of an environmentally safe, solvent-free protocol to construct the functionalized 3,4-dihydropyrimidin-2(1H)-ones/thiones. The protocol involves the three-component condensation reaction of β-keto ester, aldehyde, and urea or thiourea at elevated temperature. The key advantages of the protocol are its capacity to provide both environmental and economic benefits owing to its solvent-free conditions, short reaction times, simple workup, and good to excellent isolated yield of DHPMs.

Supporting Information



Publication History

Received: 03 October 2024

Accepted after revision: 30 December 2024

Accepted Manuscript online:
30 December 2024

Article published online:
03 February 2025

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