Transition-Metal-Free C-H Trifluoromethylthiolation of -Disubstituted Enaminones To Access CFS-Functionalized Enaminones and Their Application in the Synthesis of CFS-Heteroaryls.

The α-C-H trifluoromethylthiolation of -disubstituted enaminones has been achieved with simple and cheap CFSONa as the CFS source. The reactions were run at mild temperature (0 °C to rt) using POCl 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 CFS-functionalized enaminones have been proven as useful building blocks in the synthesis of various CFS-functionalized heteroaromatic compounds by simple annulation reactions.