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Synthesis and Antiviral Evaluation of 5-(4-Aryl-1,3-butadiyn-1-yl)-uridines and Their Phosphoramidate Pronucleotides.
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Institute of Organic and Analytical Chemistry (ICOA UMR 7311), CNRS, University of Orleans, F-45067 Orléans, France.
The emergence of RNA viruses driven by global population growth and international trade highlights the urgent need for effective antiviral agents that can inhibit viral replication. Nucleoside analogs, which mimic natural nucleotides, have shown promise in targeting RNA-dependent RNA polymerases (RdRps). Starting from protected 5-iodouridine, we report the synthesis of -substituted-(1,3-diyne)-uridines nucleosides and their phosphoramidate prodrugs.
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Shenzhen Institute of Advanced Technology, Chinese Academy of Sciences, Shenzhen 518055, P. R. China.
Sulfone motifs play important roles in bioactive compounds and functional materials. The development of efficient methodologies for constructing sulfonyl-containing compounds has thus attracted considerable attention. Here, we introduce a protocol for the preparation of alkyl aryl sulfones under mild conditions.
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National Engineering Research Center of Pesticide, College of Chemistry, Nankai University, Tianjin 300071, China.
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View Article and Find Full Text PDFHarnessing the Reactivity of Cyclopropenes in the Synthesis of Spiroketals via Putative Generation of Donor-Acceptor Cyclopropanes.
Org Lett
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Department of Chemistry, Indian Institute of Technology Bombay, Powai, Mumbai 400076, India.
Article Synopsis
- The study presents a method using TMSOTf to create spiroketal derivatives through hydroalkoxylation and cycloaddition reactions involving hydroxy cyclopropenes and aldehydes.
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Reusable Iron-Copper Catalyzed Cross-Coupling of Primary Amides with Aryl and Alkyl Halides: Access to N-Arylamides as Potential Antibacterial and Anticancer Agents.
Chemistry
December 2024
Department of Chemistry, Indian Institute of Engineering Science and Technology, Shibpur, Botanic Garden, Howrah, 711103, India.
We present, for the first time, an efficient ligand-free iron-copper catalyzed cross-coupling reaction involving a variety of aryl, heteroaryl halides (including chlorides, bromides, and iodides), and alkyl bromides with diverse aryl and aliphatic primary amides, conducted under solvent-minimized conditions. This economically competitive protocol successfully yielded the corresponding cross-coupling products, N-arylamides and N-alkylamides, in good to excellent yields with broad substrate scope (65 examples) and tolerance to several sensitive functionalities (including heterocycles). No conventional work-up is required for this protocol, and the developed method is applicable for gram-scale synthesis.
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