Abstract
As both trifluoromethylthio (CF3S) and trifluoromethoxy (CF3O) moieties have proved to be valuable functionalities in pharmaceutical chemistry, trifluoromethylthiolation and trifluoromethoxylation have received a great deal of attention. For the trifluoromethylthiolation reaction, a variety of efficient methods have been developed. Among these methods, C-H trifluoromethylthiolation avoids the need to prefunctionalize substrates, meaning that this straightforward protocol is quite attractive and promising. The first section of this review summarizes recent advances in this field, including Csp3-H, Csp2-H and Csp-H trifluoromethylthiolation and the asymmetric Csp3-H trifluoromethylthiolation reactions. Trifluoromethoxylation with safe trifluoromethoxylation reagents remains a significant challenge. The second section of this review summarizes the recent progress in trifluoromethoxylation reaction.
Keywords: C-H bond, trifluoromethylthiolation, asymmetric trifluoromethylthiolation, trifluoromethoxylation, trifluoromethoxylation reagent, fluorine.
Graphical Abstract
Call for Papers in Thematic Issues
Catalytic C-H bond activation as a tool for functionalization of heterocycles
The major topic is the functionalization of heterocycles through catalyzed C-H bond activation. The strategies based on C-H activation not only provide straightforward formation of C-C or C-X bonds but, more importantly, allow for the avoidance of pre-functionalization of one or two of the cross-coupling partners. The beneficial impact of ...read more
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