Affiliation:
1. Green Pharmaceutical Technology Key Laboratory of Luzhou City Central Nervous System Drug Key Laboratory of Sichuan Province School of Pharmacy Southwest Medical University Luzhou 646000 Sichuan People's Republic of China
2. Sichuan Provincial Center for Gynaecology and Breast Diseases The Affiliated Hospital of Southwest Medical University Luzhou 646000 Sichuan People's Republic of China
3. Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province Luzhou 646000 People's Republic of China
Abstract
AbstractAn oxidant‐free photocatalytic [2+2+m] cyclization of 2‐cyanoaryl acrylamides with 2‐bromocarbonyls is reported, enabling the assembly of biologically important N‐heterocycle‐fused quinolinones including benzo[1,6]naphthyridinones and pyrrolo[3,2‐c]‐quinolines. This photocatalytic protocol proceeds through a radical relay pathway including alkene difunctionalization along with an intramolecular cyano insertion and subsequent site‐specific functionalization of inert C(sp3)−H bond enabled by cyano‐derived iminyl radical‐mediated 1,n‐hydrogen atom transfer. Notably, this transformation selectively formed two distinct C−C bonds, one C−N bond, and one quaternary carbon center in a one‐pot procedure.
Funder
National Natural Science Foundation of China