Chemoselective Difluoromethylation of Nucleosides. [PDF]
A profiling platform to define the chemoselectivity of the carbene-mediated difluoromethylation of nucleosides is described. First, the optimized reaction conditions for the difluoromethylation of silyl-protected nucleosides are established using TMS-CF2Br and KOAc to form the difluoromethyl carbene in situ.
Linden O +3 more
europepmc +4 more sources
Dual transition metal electrocatalysis for difluoromethylation of Aryl halides using potassium difluoroacetate [PDF]
The development of robust, practical, and chemoselective methods for introducing the difluoromethyl (CF₂H) group into organic molecules is highly sought after in the fields of pharmaceutical and agrochemical design.
Naifu Zhou, Mingding Chai, Niankai Fu
doaj +2 more sources
Facile Entry to Pharmaceutically Important 3-Difluoromethyl-quinoxalin-2-ones Enabled by Visible-Light-Driven Difluoromethylation of Quinoxalin-2-ones [PDF]
CF2H moiety has a significant potential utility in drug design and discovery, and the incorporation of CF2H into biologically active molecules represents an important and efficient strategy for seeking lead compounds and drug candidates.
Kai-Zhong Fu +4 more
doaj +2 more sources
Repurposing trifluoromethyl copper (III) complexes for difluoromethylation of saccharides and complex alcohols [PDF]
Grushin’s reagent, (bpy)Cu(CF3)3, is a well-known trifluoromethylation agent, but its potential as a difluorocarbene source has remained largely unexplored.
Shuolu Dai +7 more
doaj +2 more sources
Ball-Milling Assisted Iron-Catalyzed Difluoromethylation Toward the Synthesis of Valuable Oxindoles. [PDF]
An iron‐catalyzed difluoroalkylation of acrylamides under ball‐milling conditions affords oxindoles in up to 85% yield. Analytical studies reveal that the apparent piezoelectric activity originates from iron leaching caused by milling assembly abrasion during the reaction process. The iron‐catalyzed process proves to be efficient with a broad substrate
Solomin V +4 more
europepmc +2 more sources
Defluoroalkylation of Trifluoromethane with Organolithium Reagents: Mechanism and Synthesis of Fluoroalkenes. [PDF]
We report a rare example of the transformation of HCF3 into a fluoroalkene functional group through defluoroalkylation. We rationalise product formation through DFT calculations, scale‐up the synthesis through continuous flow methods, and show that a fluoroalkene reagent derived from HCF3 is a competent nucleophile for the fluoroethenylation of a range
Warsame HR +4 more
europepmc +3 more sources
Synthetic Strategies to Access Fluorinated Azoles. [PDF]
This review highlights recent synthetic strategies for introducing fluorine groups (mono‐, di‐, and trifluoromethylation) into 11 major azole classes, identifying research gaps to inform future innovations in materials science, medicinal chemistry, and biomedical research.
El-Gaber MKA +4 more
europepmc +2 more sources
Advances in the Different Synthetic Routes of Fluorinated Hydrazines. [PDF]
This review highlights the various routes to the preparation of fluorinated hydrazines, thereby promoting the exploration of innovative methods for the synthesis of new N‐fluorinated hydrazines. Their synthesis mainly involves synthetic routes such as organometallic, organocatalytic, and photocatalytic.
Kyrko D, Crousse B.
europepmc +2 more sources
Mechanochemical difluoromethylations of ketones. [PDF]
We present a mechanochemical synthesis of difluoromethyl enol ethers. Utilizing an in situ generation of difluorocarbenes, ketones are efficiently converted to the target products under solvent-free conditions. The reactions proceed at room temperature and are complete within 90 minutes, demonstrating both efficiency and experimental simplicity.
Ke J, van Bonn P, Bolm C.
europepmc +4 more sources
Introduction of the difluoromethyl group at the meta- or para-position of pyridines through regioselectivity switch [PDF]
Difluoromethyl pyridines have gained significant attention in medicinal and agricultural chemistry. The direct C−H-difluoromethylation of pyridines represents a highly efficient economic way to access these azines.
Pengwei Xu +3 more
doaj +2 more sources

