Unsaturated -sulfonyl amidines are transformed into valuable N-heterocyclic products when heated with BFOTf. Mechanism studies suggest a domino 1,7-H shift, activating a C-H bond, followed by electrocylisation that results in stereodefined cyclic amidines.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1039/d3cc01127e | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Alternative and Sustainable Route to Explore a New Class of Amidines by Photochemical Synergistic Effect of Copper/Nitroxyl Radical Catalysis via Halogen-Atom Transfer.
Chemistry
January 2025
VIT University, Materials Chemistry Division, School of Advanced Sciences, VIT University, 632014, Vellore, INDIA.
Amidines are a vital class of bioactive compounds and often necessitate multiple components for their synthesis. Therefore, exploring efficient and sustainable methodologies for their synthesis is indispensable. Herein, we disclose an alternative and greener method for synthesizing an unexplored new class of amidines through the photochemical synergistic effect of copper/nitroxyl radical catalysis.
View Article and Find Full Text PDFIn silico and in vitro evaluation of the potential genotoxic impurities of vildagliptin.
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Department of Toxicology, Faculty of Pharmacy, Yeditepe University, 34755, Ataşehir, Istanbul, Turkey.
Establishing the safety of impurities in drug substances or products is crucial. The assessment of genotoxicity for these impurities and determining the acceptable limits pose considerable challenges, as recognized in recent guidelines. While the genotoxicity profile of vildagliptin-an oral hypoglycemic drug-is well established, there is limited knowledge about the genotoxic potential of its impurities.
View Article and Find Full Text PDFHalide-free ion pair organocatalyst from biobased α-hydroxy acid for cycloaddition of CO to epoxide.
Org Biomol Chem
January 2025
State Key Laboratory Materials-Oriented Chemical Engineering, College of Biotechnology and Pharmaceutical Engineering, Nanjing Tech University, 30 Puzhu Road South, Nanjing 211816, China.
The cycloaddition of CO to epoxide (CCE) reactions produce valuable cyclic carbonates useful in the electrolytes of lithium-ion batteries, as organic solvents, and in polymeric materials. However, halide-containing catalysts are predominantly used in these reactions, despite halides being notoriously corrosive to steel processing equipment and residual halides also having harmful effects. To eliminate the reliance on halides as cocatalyst in most CCE reactions, halide-free catalysts are highly desirable.
View Article and Find Full Text PDFSynthesis and in vitro leishmanicidal activity of novel N-arylspermidine derivatives.
Bioorg Chem
January 2025
Universidad de Buenos Aires, CONICET, Cátedra de Química Orgánica II, Departamento de Ciencias Químicas, Facultad de Farmacia y Bioquímica, Junín 956, 1113 Buenos Aires, Argentina. Electronic address:
Article Synopsis
- The study focuses on creating and testing new N-arylspermidine derivatives for their effectiveness against Leishmania infantum, a parasite causing a neglected tropical disease.
- These compounds were synthesized through a unique method involving cyclic amidines, demonstrating good potential with eight out of ten showing effective ecological concentrations (EC) against the parasite's intracellular form.
- Two derivatives, 3b and 3h, exhibited comparable efficacy to the existing treatment Miltefosine, indicating promising candidates for further development and optimization in treating Leishmania infections.
cGAS/STING pathway modulation in polyhexamethyleneguanidine phosphate-induced immune dysregulation and pulmonary fibrosis using human monocytic cells (THP-1) and male C57BL/6 mice.
J Toxicol Environ Health A
February 2025
College of Pharmacy, The Catholic University of Korea, Bucheon, Republic of Korea.
Polyhexamethyleneguanidine phosphate (PHMG), a widely used antimicrobial agent, has been implicated in humidifier disinfectant-associated lung injuries (HDLI). PHMG exposure suppressed interferon regulatory factor 3 (IRF3) activation and interferon-β (IFN-β) expression induced by a cGAS agonist or a STING agonist in human monocytic cells (THP-1), which are known to transition to alveolar macrophages during pulmonary fibrosis development. However, the mechanisms underlying PHMG-induced pulmonary toxicity in lung remain unclear.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!