The trifluoromethyl group, a unique functional group that exhibits profound physical and chemical properties, is increasingly popular in various areas, especially the pharmaceutical and agrochemical industries. Therefore numerous methodologies have been developed, trying to achieve the selective incorporation of trifluoromethyl group. Among the existing methods to construct C-CF3 bonds, radical trifluoromethylation reactions have received much more attention due to their high reactivity, mild reaction condition, and wide substrate scope. In this work we present a radical (bis)trifluoromethylation-cyclization reaction of 1,6-enyne substrates with the assistance of a novel trifluoromethylated Cu(III) complex. Applying simple and mild reaction conditions, we are able to construct C-CF<sub>3</sub> and C-C bonds across a set of various unsaturated moieties with outstanding chemoselectivity and stereoselectivity, providing more potential for the synthesis and structural study of trimethylated compounds with more complex skeletons.

Copper mediated (bis)trifluoromethylation–cyclization cascade reaction

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