This review will be an essential toolbox for medicinal and bioorganic chemists seeking novel multifunctional hybrid and bioactive N-heterocycles for drug discovery. The work highlights the need for and relevance of unexplored bioisosterism employing isoquinoline-based small-molecules in drug design.
An unprecedented de novo synthetic strategy for the construction of C–O axially chiral aryl-heterocyclic ethers was developed via a cobalt-catalyzed asymmetric C–H activation/annulation of arylamides with rationally designed phenylethynyl ethers.
Photo-induced copper salt-mediated cascade C–C and C–N/O bond formations for the synthesis of isocoumarin and isoquinolinone derivatives at room temperature.
A series of phenolic isoquinolinones with dual action (antioxidant and α-glucosidase inhibition) is shown for the first time. In vivo assays also demonstrate the reduction of blood glucose after administration of sucrose.
An efficient metal-free approach for the synthesis of isoindolinones and isoquinolinones from 1,2,3-benzotriazin-4(3H)-ones via electron donor–acceptor (EDA) complex formation under visible light is described.