Practical and modular construction of benzo[c]phenanthridine compounds

Abstract Here, we describe a general and modular strategy for the rapid assembly of benzo[ c ]phenanthridine (BCP) derivatives using homogeneous gold catalysis. Notably, in contrast to traditional methods based on specially preformed substrates that have an inherent preference formation this class compounds with limited flexibility, protocol is achieved via selectively intramolecular cascade diazo-tethered alkyne subsequently intermolecular cyclization nitrile facilitate successive C-N C-C bonds formation. This methodology uses readily available nitriles as nitrogen source deliver products good yield excellent functional group compatibility. A preliminary anti-tumor activity study these generated exhibits high anticancer potency against five tumor cell lines, including HeLa, Mel624, SW-480, 8505C, LAN-1. Besides, report catalyst-controlled cycloaddition/intramolecular insertion substrate fulvene provide fused polycarbocycles containing seven-membered ring.