Synthetic Strategies for Deuterated Fluorocarbon Moieties
Ye Lin , Tsz Chun Lee , Jinglin Ma , Tianbo Wang , Yan Li , Wai Chung Fu
Chinese Journal of Chemistry ›› 2026, Vol. 44 ›› Issue (11) : 1876 -1894.
Deuterated fluorocarbon moieties such as CF2D uniquely merge fluorine's lipophilicity and metabolic benefits with deuterium's kinetic isotope effect, and offer unprecedented and underexplored possibilities in future drug design and medicinal chemistry research. However, persistent challenges include low deuterium incorporation levels, lengthy synthetic routes, inaccessible precursor reagents, and selectivity issues have historically limited the exploration of these motifs in medicinal chemistry and drug discovery. Since 2017, efficient synthetic methods achieving consistently high deuterium incorporation levels have emerged, and diverse mechanistic approaches were developed to enable mild and selective preparation of a wide range of deuterated fluorocarbon compounds. A series of bench-stable, versatile reagents were disclosed to promote incorporation of deuterated fluorocarbon motifs. These advancements underscore the growing potential of deuterated fluorocarbon motifs in drug discovery and beyond.
Deuterated pharmaceuticals / Fluorine-containing drugs / Late-stage functionalization / Medicinal chemistry / Organofluorine chemistry / Difluoromethyl group / Difluorocarbene / Deuterodefluorination
2026 SIOC, CAS, Shanghai, & WILEY-VCH GmbH
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