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The synthesis of tetra-substituted pyrazoles holds significant synthetic value and has been accomplished through an organo-photocatalyzed decarboxylative intramolecular cyclization using readily available 1,2-diaza-1,3-dienes and α-ketoacids. This method allows for the systematic synthesis of substituted pyrazole derivatives. Notably, this approach is characterized by its metal-free and oxidant-free nature, offering distinct advantages such as short reaction times and exceptionally mild reaction conditions. The developed methodology enables the efficient construction of tetra-substituted pyrazoles, expanding the available chemical space for exploration and opening up potential applications in various scientific fields.
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http://dx.doi.org/10.1039/d4ob00248b | DOI Listing |
Molecules
July 2025
Department of Organic Chemistry, Institute of Chemistry, Federal Rural University of Rio de Janeiro, Seropédica 23897-000, RJ, Brazil.
Three previously synthesized ketene dithioacetals were used as intermediates to obtain four nucleophiles to synthesize ten tetra-substituted pyrazoles (-). This was achieved through microwave irradiation in ethanol as the solvent, yielding superb results ranging from 68.4% to 90.
View Article and Find Full Text PDFBioorg Chem
July 2025
Department of Chemistry, IB College Panipat, Haryana 132103, India.
Diabetes rank among the most critical health challenges globally. Consequently, the development of therapeutic agents targeting this health issue has become a focal point for researchers worldwide. To achieve this, tetra substituted pyrazoles were synthesized in two steps: initially, thiolated diketones were prepared using NaOH/KI catalysed approach in acetonitrile.
View Article and Find Full Text PDFACS Pharmacol Transl Sci
August 2024
Institute of Biochemistry and Molecular Medicine, University of Bern, Bern 3012, Switzerland.
The cannabinoid CB2 receptor (CB2R) is a potential therapeutic target for distinct forms of tissue injury and inflammatory diseases. To thoroughly investigate the role of CB2R in pathophysiological conditions and for target validation , optimal pharmacological tool compounds are essential. Despite the sizable progress in the generation of potent and selective CB2R ligands, pharmacokinetic parameters are often neglected for studies.
View Article and Find Full Text PDFbioRxiv
April 2024
Institute of Biochemistry and Molecular Medicine, University of Bern, Bern 3012, Switzerland.
The cannabinoid CB2 receptor (CB2R) is a potential therapeutic target for distinct forms of tissue injury and inflammatory diseases. To thoroughly investigate the role of CB2R in pathophysiological conditions and for target validation , optimal pharmacological tool compounds are essential. Despite the sizable progress in the generation of potent and selective CB2R ligands, pharmacokinetic parameters are often neglected for studies.
View Article and Find Full Text PDFOrg Biomol Chem
March 2024
Department of Chemical Sciences, Indian Institute of Science Education and Research Kolkata, Mohanpur, West Bengal 741246, India.