Copper-catalyzed domino cyclization of anilines and cyclobutanone oxime: a scalable and versatile route to spirotetrahydroquinoline derivatives

• Qingqing Jiang,
• Xinyi Lei,
• Pan Gao and
• Yu Yuan

Beilstein J. Org. Chem. 2025, 21, 749–754, doi:10.3762/bjoc.21.58

• the desired product. Keywords: copper catalysis; cyclobutane-fused tetrahydroquinolines; domino cyclization reaction; green synthesis; Introduction Tetrahydroquinolines (THQs) represent a privileged scaffold in medicinal chemistry, exhibiting a broad spectrum of biological activities and serving as

• utility and scalability [9][10][11][12][13][14][15][16][17][18][19][20]. Cyclobutane-fused tetrahydroquinolines (THQs) have garnered significant attention in drug discovery due to their inherent structural rigidity and enhanced pharmacological profiles [21], which render them highly desirable for

• the growing significance of cyclobutane-fused tetrahydroquinolines (THQs) in biochemistry and medicinal chemistry [26][27][28], we have developed an efficient and convenient method for synthesizing cyclobutane-fused and conformationally constrained spirotetrahydroquinolines (STHQs) from arylamines and