A simple one-pot procedure for the iminium salt formation: an efficient route to β-arylethylamines

A practical and highly efficient process for the preparation of β-arylethylamines 7 was developed. Benzylic organozinc compounds 10 were reacted with the iminium salts 9 generated in situ from the amine salt 8 and paraformaldehyde in one pot and in a polar and aprotic solvent, such as NMP. A variety of the β-arylethylamines were prepared in 43–91% yields.