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,
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