A rapid and efficient method for 'one-pot' synthesis of pyrazoles from (hetero)arenes and carboxylic acids via successive formation of ketones and β-diketones followed by heterocyclization with hydrazine has been developed. The utility of the RCOOH/TfOH/TFAA acylation system for intermediate production of ketones and 1,3-diketones is a key feature of this approach. The preliminary evaluation of the anticancer activity of the synthesized pyrazoles is performed.
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http://dx.doi.org/10.1039/d0ob01228a | DOI Listing |
Acc Chem Res
January 2025
Department of Chemistry and Research Center for Chemical Biology and Omics Analysis, College of Science, Southern University of Science and Technology, Shenzhen 518055, China.
ConspectusThe advancement of synthetic methodologies is fundamentally driven by a deeper understanding of the structure-reactivity relationships of reactive key intermediates. Carbyne anions are compounds featuring a monovalent anionic carbon possessing four nonbonding valence electrons, which were historically confined to theoretical constructs or observed solely within the environment of gas-phase studies. These species possess potential for applications across diverse domains of synthetic chemistry and ancillary fields.
View Article and Find Full Text PDFJ Org Chem
January 2025
Laboratory of Pharmaceutical Chemistry, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8412, Japan.
A one-pot, telescoped transformation of silyl ethers into cyanides that proceeds via silyl-ether oxidation mediated by nitroxyl-radical catalyst and [bis(trifluoroacetoxy)iodo]benzene followed by an imine formation-oxidation sequence using iodine and aqueous ammonia is reported. This transformation is effective for the site-selective transformation of benzylic and allylic silyl ethers in the presence of other silyl ethers. Using an -protected oxime and a catalytic amount of triflic acid instead of iodine/aqueous ammonia is also effective for cyanation.
View Article and Find Full Text PDFACS Catal
January 2025
Fakultät für Chemie und Pharmazie, Universität Regensburg, Regensburg 93040, Germany.
Transition metal catalysis is crucial for the synthesis of complex molecules, with ligands and bases playing a pivotal role in optimizing cross-coupling reactions. Despite advancements in ligand design and base selection, achieving effective synergy between these components remains challenging. We present here a general approach to nickel-catalyzed photoredox reactions employing -butylamine as a cost-effective bifunctional additive, acting as the base and ligand.
View Article and Find Full Text PDFMacromol Rapid Commun
January 2025
Department of Chemistry, Imperial College London, Molecular Sciences Research Hub, White City Campus, Wood Lane, London, W12 0BZ, UK.
A novel PLGA-inspired NP polymerization technique is presented, which allows the formation of NPs via the cross-linking of precisely sequenced short oligolactoglycolic acid dimethacrylates (OLGADMAs). Following the synthesis of a range of OLGADMAs, a library of NPs via this rapid and surfactant-free nanopolymerization method is successfully generated, which permits the simultaneous NP formation and encapsulation of drugs such as dexamethasone. The results indicate that NPs produced through this nanopolymerization technique with precisely controlled sequences exhibit heightened stability compared to conventionally sequenced and non-sequence controlled PLGA, as evidenced by minimal pH changes over five weeks.
View Article and Find Full Text PDFSci Rep
January 2025
Nanomaterials Science Research Laboratory, Chemistry Department, Faculty of Science, Beni-Suef University, Beni-Suef, Egypt.
The design and fabrication of novel electrodes with strong electrochemical responses are crucial in advanced supercapacitor technology. In this study, a poly(m-toluidine)/silver-silver oxide (PMT/Ag-AgO) nanocomposite was prepared using the photopolymerization method. Various characterization techniques were employed to analyze the prepared nanomaterials.
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