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An improved synthesis of the antiviral drug adefovir is presented. Problems associated with current routes to adefovir include capricious yields and a reliance on problematic reagents and solvents, such as magnesium -butoxide and DMF, to achieve high conversions to the target. A systematic study within our laboratory led to the identification of an iodide reagent which affords higher yields than previous approaches and allows for reactions to be conducted up to 10 g in scale under milder conditions. The use of a novel tetrabutylammonium salt of adenine facilitates alkylations in solvents other than DMF. Additionally, we have investigated how regioselectivity is affected by the substitution pattern of the nucleobase. Finally, this chemistry was successfully applied to the synthesis of several new adefovir analogues, highlighting the versatility of our approach.
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http://dx.doi.org/10.3762/bjoc.15.77 | DOI Listing |
Chemistry
March 2025
Universitaet Kiel, Institut fuer Organische Chemie, Otto-Hahn-Platz 4, 24118, Kiel, GERMANY.
Diazocines are bridged azobenzenes with improved photophysical properties. One of the main features is the fact that, unlike the azobenzenes, the Z form is more stable than the E isomer. Another important property is the more rigid structure (tricyclic), which precisely defines the molecular movement.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
March 2025
Northeast Normal University, School of Chemistry, CHINA.
Photosynthesis of hydrogen peroxide from earth-abundant water and air over organo-based semiconducting materials is a promising alternative to the traditional anthraquinone (AQ) method. However, the generally hydrophobic nature of organic semiconductors has led to their poor dispersibilities in aqueous systems, which built huge barriers for photon capture and reactant contact in water-based photocatalysis. Aiming at this issue, this study reports the facile synthesis of AQ-based porous aromatic frameworks (AQ-PAFs) by coupling of AQ fragments with thiophene-derived linkers via robust carbon-carbon bonds.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
March 2025
Dalian University of Technology, State Key Leb of Fine Chemicals, No 2 Linggong Road, Gaoxin District, 116024, Dalian, CHINA.
One-pot synthesis of glycol from ethylene and H2O2 is simple and environmentally friendly, making it a potential alternative for glycol production. The key to the success of this is to have a bifunctional catalyst with both oxidative activity for ethylene in the presence of H2O2 and acidic centers for the subsequent hydration of ethylene oxide. Here, we propose a dual-chemical post-treatment regime to introduce acid centers in TS-1 while simultaneously improve the oxidative activity.
View Article and Find Full Text PDFJ Neuroendocrinol
March 2025
Department of Zoology, University of Allahabad, Prayagraj, India.
Extra-retinal photoreception is common across fish and avian species. In birds, the hypothalamus contains non-visual photoreceptors that detect light and regulate multiple endocrine systems. To date, light-dependent control of seasonal reproduction is one of the most well-studied systems that require deep brain photoreception.
View Article and Find Full Text PDFISA Trans
March 2025
School of Electrical Engineering and Computer Science, National University of Sciences and Technology (NUST), Islamabad, Pakistan. Electronic address:
Glucose acts as a fundamental energy source for cells and plays a pivotal role in various physiological processes, including metabolism, signaling, and cellular control. Maintaining precise regulation of blood glucose levels is crucial for overall health and equilibrium. To achieve this balance, insulin is administered either orally or through an artificial pancreas (AP) during sleep, utilizing control algorithms based on mathematical models to regulate blood glucose concentration (BGC).
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!