Catalytic Trifluoromethylthiolation Using N-(Trifluoromethylthio)phthalimide

Rueping et al. have reported the catalytic trifluoromethylthiolation using N-(trifluoromethylthio)phthalimide (1). According to their results, 1 acts as an electrophilic source of CF₃S⁺, and readily reacts with boronic acids and terminal alkynes under copper catalysis to afford the corresponding CF₃S group containing compounds. 1 is a useful trifluoromethylthiolating agent, because it is shelf-stable and easy-to-handle, and the reaction proceeds under mild conditions. Now, the studies of the biological activities of CF₃S group substituted compounds are attracting interest. So, 1 is expected to be applied for the synthesis of bioactive compounds as well as pharmaceutical and agrochemical research.