The α-C–H trifluoromethylthiolation of N,N-disubstituted enaminones has been achieved with simple
and cheap
CF3SO2Na as the CF3S source. The
reactions were run at mild temperature (0 °C to rt) using POCl3 as the only reducing reagent. The work represents the first
example on the synthesis of α-trifluoromethylthio
enaminones via direct C–H functionalization. In addition, the
resulting CF3S-functionalized enaminones have been proven
as useful building blocks in the synthesis of various CF3S-functionalized heteroaromatic compounds by simple annulation reactions.