Copper-catalyzed intermolecular and regioselective aminofluorination of styrenes: facile access to beta-fluoro-N-protected phenethylamines

A copper-catalyzed regio-and intermolecular aminofluorination of styrenes has been developed. In this reaction Ph-I=N-Ts and Et3N center dot 3HF act as nitrogen and fluorine sources, respectively. The obtained beta-fluoro-N-Ts-phenethylamines can be N-alkylated with subsequent deprotection affording the corresponding beta-fluoro-N-alkylated phenethylamines, which are interesting building blocks for compounds acting on neuronal targets.