An alkylation of C-H bonds with maleimides by a rhodium-catalyzed reaction of aromatic amides containing an 8-aminoquinoline moiety as the directing group is reported. Various N-substituents in the maleimide, including methyl, ethyl, cyclohexyl, benzyl, and phenyl groups and even H, are applicable to the reaction. The reaction is highly regioselective at the less hindered ortho-C-H bond when meta-substituted aromatic amides are used as substrates.
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http://dx.doi.org/10.1021/acs.orglett.7b02135 | DOI Listing |
J Biochem Mol Toxicol
January 2025
Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, Guwahati, India.
This study is focused on the design, synthesis, and evaluation of some sulfonamide derivatives for their inhibitory effects on human carbonic anhydrase (hCA) enzymes I, II, IX, and XII as well as for their antioxidant activity. The purity of the synthesized molecules was confirmed by the HPLC purity analysis and was found in the range of 93%-100%. The inhibition constant (K) against hCA I ranged from 0.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
January 2025
Universitat Bern, Department of Chemistry and Biochemistry, Freiestrasse 3, 3012, Bern, SWITZERLAND.
Isotope Exchange processes are becoming the preferred way to prepare isotopically labelled molecules, avoiding the redesign of multistep synthetic protocols. In the case of deuterium incorporation, the most used strategy has employed transition metals, that offer high reactivity under mild reaction conditions. Despite their success, the trade-off is that these metals are precious, and often exhibit high toxicity.
View Article and Find Full Text PDFNutrients
December 2024
Department of Pharmacognosy, Faculty of Pharmacy, "Iuliu Haţieganu" University of Medicine and Pharmacy, 400010 Cluj-Napoca, Romania.
Background/aim: L. () is an aromatic medicinal species with important nutraceutical potential, having rosmarinic acid (RA) as one of its main metabolites. The present study aims to evaluate the effects of an extract obtained from the leaves of this species and of its main metabolite in improving the streptozotocin-induced damage of hearts and aorta of diabetic rats.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
January 2025
The University of Manchester, School of Chemistry & Manchester Institute of Biotechnology, 131 Princess Street, M1 7DN, Manchester, UNITED KINGDOM OF GREAT BRITAIN AND NORTHERN IRELAND.
Amide bond formation is fundamental in nature and is widely used in the synthesis of pharmaceuticals and other valuable products. Current methods for amide synthesis are often step and atom inefficient, requiring the use of protecting groups, deleterious reagents and organic solvents that create significant waste. The development of cleaner and more efficient catalytic methods for amide synthesis remains an urgent unmet need.
View Article and Find Full Text PDFJ Chromatogr A
December 2024
Univ Rouen Normandie, FR3038, SMS, UR 3233, F-76000 Rouen, France. Electronic address:
In this study, a novel imidazolium-based ionic liquid (IL) coating was developed for stir bar sorptive extraction (SBSE) using a sol-gel method. The effects of different counterions, conditioning temperatures and polymer compositions were investigated. The stir bar with bis((trifluoromethyl)sulfonyl) amide 1-butyl-3-(3-(triethoxysilyl)propyl)-1H-imidazol-3-ium showed good mechanical and thermal stability with high resistance to water solubilization.
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