Convenient synthesis of 8‐aryl‐6‐aryl‐1,2,3,4‐tetrahydroisoquinoline‐5,7‐dicarbonitriles via a cascade Michael/cyclization reaction

Abstract

A convenient and straightforward cascade Michael/cyclization reaction of 1‐alkylpiperidin‐4‐ones, acyl acetonitriles, and aldehydes was proposed for the construction of significant 8‐aryl‐6‐aryl‐1,2,3,4‐tetrahydroisoquinoline‐5,7‐dicarbonitriles promoted by DBU, and various 8‐aryl‐6‐aryl‐1,2,3,4‐tetrahydroisoquinoline‐5,7‐dicarbonitrile derivatives were produced in medium to high yields. The methodology features a simple operation process, accessible raw material, and high atomic economy.