One well-known multicomponent reaction that is helpful in the synthesis of dihydropyrimidinones (DHPMs), important molecules in organic synthesis and medicinal chemistry, is the Biginelli reaction. Because of their wide range of biological activities, DHPMs are regarded as essential chemicals. A great deal of research has been done in the last few decades to find ways to produce enantiomerically pure DHPMs because of their notable and focused target-oriented biological activities. In this reaction, numerous structural variants and catalysts have been employed in a range of solvents to yield an enormous number of Biginelli-type compounds. In the present review, the available catalysts in the literature including ionic liquids, Lewis acids, and organocatalysts for the Biginelli reaction and synthesis of a large number of asymmetric compounds since 2003 are summarized.
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http://dx.doi.org/10.1007/s11030-024-10827-7 | DOI Listing |
Sci Rep
January 2025
Natural and Medical Sciences Research Center, University of Nizwa, P.O. Box 33, 616, Birkat Al Mauz, Nizwa, Sultanate of Oman.
In this research, with the Green Chemistry approach, to load more sulfonic acid active sites on catalyst surfaces, a nanocomposite material based on core-shell magnetite coated with vinyl silane and a sulfonated polymeric brush-like structure is designed and synthesized as a new class of efficient solid acid catalysts, referred to as FeO@VS-APS brush solid acid. The synthesized catalyst was comprehensively characterized by a range of instrumental techniques, including XRD, SEM, TEM, FT-IR, EDX, TGA, and VSM. The activity of the catalyst was evaluated in Biginelli, Strecker, and esterification reactions.
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December 2024
Department of Chemistry, National Institute of Technology Karnataka (NITK) Surathkal Mangalore-575025 India
3,4-Dihydropyrimidin-2(1)-ones (DHPMs) and 1,4-dihydropyridines (DHPs), prepared by applying the Biginelli and Hantzsch reaction protocols, respectively, are well-documented nitrogen-containing heterocycles with intriguing pharmacological properties. The aqueous solution of biogenic carboxylic acids renewably produced from biomass catalytic or enzymatic processes can be used as a sustainable catalyst and green reaction media for synthesizing DHPs and DHPMs. This work evaluates the efficacy of various biogenic acids in their aqueous solutions as catalysts for synthesizing DHPs and DHPMs from substituted benzaldehydes.
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January 2025
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
Heliyon
October 2024
Jai Research Foundation, Valvada, Vapi, Gujarat, 396105, India.
The paper describes the construction of a new series of pyrimidinone-linked thiazole derivatives through bromination of the initial Biginelli reaction product followed by the Hantzsch thiazole synthesis route. Various analytical techniques, including FT-IR, H NMR, C NMR, and LCMS analysis, were employed to confirm the formation of the products. The synthesized compounds were primarily evaluated for their antibacterial activity, with a specific focus on their IC values.
View Article and Find Full Text PDFBioorg Chem
December 2024
Department of Science, Institute for Information Technologies Kragujevac, University of Kragujevac, Kragujevac 34000, Serbia. Electronic address:
The aim of the presented research was to explore anticancer potential of eleven newly synthesized tetrahydropyrimidine derivatives. The compounds were synthesized via Biginelli multicomponent one-pot reaction using different derivatives of vanillin, ethyl 4-chloroacetoacetate and (N-methyl)urea. The cytotoxic effects of the compounds were examined on three human malignant cell lines (HeLa, K562, and MCF7), and normal lung fibroblasts MRC-5.
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