The first three-component coupling reactions between various anilines (1), benzaldehydes (2), and cyclohexen- 2-one (3) were performed under mild conditions (acetonitrile, room temperature, 14 h) in the presence of 20 mol % BiCl3 to obtain new 2,3-diaryl-2-aza[2.2.2]octan-5-ones (4,5) with interesting acetylcholinesterase inhibitory properties. Keywords: 2,3-Diaryl-2-azabicyclo[2.2.2]octan-5-one, catalysed three-component aza Diels-Alder reaction, acetylcholinesterase inhibitors