An operationally simple and concise synthesis of anilinoethanolamines, as NMDA NR2B receptor antagonist ifenprodil analogues, was developed via a copper-catalyzed amination of the corresponding bromoarene. Coupling was achieved with linear primary alkylamines, α,ω-diamines, hexanolamine and benzophenone imine, as well as with aqueous ammonia, in good yields using CuI and N,N-diethylsalicylamide, 2,4-pentadione or 2-acetylcyclohexanone as catalytic systems. Amination with ethylene diamine was efficient even in the absence of an additive ligand, whereas no reaction occurred with ethanolamine whatever the conditions used. The anilinoethanolamines were evaluated as NR2B receptor antagonists in a functional inhibition assay. Aminoethylanilines displayed inhibition effects close to that of ifenprodil.

Sultones were subject to ring opening by nucleophilic attack with [¹⁸F]fluoride to afford easily purified ¹⁸F-labelled hydrophilic sulfonated products in high yields. A two-step sequence including radiofluorination and coupling to lysine was then developed from a bis-sultone precursor as a model approach for the labelling of biopolymers.

The ¹¹C-monomethylstannate prepared from [¹¹C]-methyl iodide and Lappert's stannylene, was subject to a palladium-mediated cross-coupling reaction with an aryl halide under ligand-free conditions, to afford easily purified ¹¹C-methyl(hetero)arenes in high radiochemical yields.

[ ¹⁸ F]-Fluoride ready for SNAr was prepared according to a simple process including trapping of aqueous [ ¹⁸ F]-fluoride on a cartridge pre-loaded with the phosphonium borane [(Ph ₂ MeP)C ₆ H ₄ (BMes ₂ )] ⁺ , then releasing by elution of TBACN in dry acetonitrile.