The mild and fast copper‐catalyzed radical and regioselective aminoalkoxylation of styrenes by using N‐fluorobenzenesulfonimide and simple alcohols as nitrogen and alkoxy sources, respectively, was investigated. The aminoalkoxylated products obtained could be used in the synthesis of new compounds with possible activity as neurotransmitter receptor ligands.

An efficient, regioselective and rapid copper-catalyzed one-pot aminoalkoxylation of styrenes has been developed using different alcohols and phenyl iminoiodinanes.

The utility of the method is demonstrated by its application in the synthesis of an analogue [cf.(XIa)] of the commercial antidepressant fluoxetine [cf.(XIb)]