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
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
Electrosynthesis of 1,1-Bis(difluoromethyl)alkenes via Twofold C−H Difluoromethylation as Bioisosteres of Elusive 1,1-Enediols [PDF]
Geminal bis(difluoromethyl)alkenes, featuring two CF2H groups as lipophilic hydrogen-bond donor surrogates, are highly coveted yet rarely accessible bioisosteres of 1,1-enediols that remain nearly theoretical due to their inherent instability.
Seonyoung Kim +5 more
doaj +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
Metallaphotoredox Difluoromethylation of Aryl Bromides [PDF]
AbstractHerein, we report a convenient and broadly applicable strategy for the difluoromethylation of aryl bromides by metallaphotoredox catalysis. Bromodifluoromethane, a simple and commercially available alkyl halide, is harnessed as an effective source of difluoromethyl radical by silyl‐radical‐mediated halogen abstraction.
Masaru Kondo +2 more
exaly +3 more sources
Visible-light-promoted radical cyclisation of unactivated alkenes in benzimidazoles: synthesis of difluoromethyl- and aryldifluoromethyl-substituted polycyclic imidazoles [PDF]
An efficient and eco-friendly approach for synthesizing difluoromethyl- and aryldifluoromethyl-substituted polycyclic imidazoles was established via a visible-light-promoted radical cyclization reaction.
Yujun Pang +5 more
doaj +2 more sources
Development of a halofluorocarbon, chromatography-free radiosynthesis of fluorine-18 difluorocarbene [PDF]
Background In recent years, the development of the [18F]difluoromethyl radical ([18F]2-((difluoromethyl)sulfonyl)benzo[d]thiazole, [18F]4), and [18F]difluorocarbene ([18F]1-chloro-4-((difluoromethyl)sulfonyl)benzene, [18F]10) prosthetic groups, has paved
Catherine G. F. Dickmann +3 more
doaj +2 more sources
1,6-Nucleophilic Di- and Trifluoromethylation of para-Quinone Methides with Me3SiCF2H/Me3SiCF3 Facilitated by CsF/18-Crown-6 [PDF]
The direct 1,6-nucleophilic difluoromethylation, trifluoromethylation, and difluoroalkylation of para-quinone methides (p-QMs) with Me3SiRf (Rf = CF2H, CF3, CF2CF3, CF2COOEt, and CF2SPh) under mild conditions are described. Although Me3SiCF2H shows lower
Dingben Chen +7 more
doaj +2 more sources

