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Methods for trifluoromethylthiolation are very limited. To tackle this problem, a mild and efficient approach to the 2-trifluoromethylthiolation of glycals has been developed. This protocol employed N-trifluoromethylthiosaccharin as the trifluoromethylthiolating reagent, TMSCl as the activator, and DBU as the base, affording 2-trifluoromethylthioglycals in good yields. These trifluoromethylthiolated carbohydrates may benefit the development of carbohydrate-based drugs.

Graphical abstract: 2-Trifluoromethylthiolation of glycals

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