Tetrahydrofuranylmethylamines: An efficient and simple one‐step synthesis and biological activities

Various tetrahydrofuran‐2‐ylmethylamines have been prepared in good yields by an efficient one‐step synthesis utilizing the reaction of tetrahydrofurfurylchloride with different secondary cyclic amines without any catalyst. The compounds were tested for their in vitro affinity for the (α4)₂(β2)₃ and α7* nicotinic acetylcholine receptor (nAChR) subtypes. Pyrrolidine, piperidine and azepane containing analogs ( 1a, 1b, 1c ) showed K_i values in the lower micromolar range for these neuronal nAChR subtypes in rat brain.