Nucleophilic triﬂuoromethoxylation of alkyl halides without silver
The biological properties of molecules containing the triﬂuoromethoxy group have made these compounds important targets in pharmaceuticals and agrochemicals, yet their preparation is still a substantial challenge. Herein, we present a practical nucleophilic triﬂuoromethoxylation of alkyl halides with (E)-O-triﬂuoromethyl-benzaldoximes (TFBO) as a triﬂuoromethoxylation reagent in the absence of silver under mild reaction conditions. The triﬂuoromethoxylation reagent TFBO is easily prepared and thermally stable, and can release CF3O.
species in the presence of a base. Furthermore, broad scope and good functional group compatibility are demonstrated by application of the method to the late-stage triﬂuoromethoxylation of alkyl halides in complex small molecules.