2-Trifluoromethylthiolation of glycals. Issue 27 (13th June 2016) - Yu, Yang
Abstract : The direct 2-trifluoromethylthiolation of glycals has been realized for the first time, benefiting the carbohydrate-based drug discovery. Abstract : 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.