Hellgren Victor, Singh Pardeep, Kulkarni Abhilash, Bagheri Niusha, Widengren Jerker, Manavalan Gopinathan, Almqvist Fredrik
Department of Chemistry, Umeå University, SE-90187 Umeå, Sweden.
Department of Applied Physics, Royal Institute of Technology (KTH), SE-10691 Stockholm, Sweden.
J Org Chem. 2024 Aug 16;89(16):11802-11810. doi: 10.1021/acs.joc.4c01224. Epub 2024 Jul 25.
We have developed an Ir(PPy) photoredox-catalyzed cross-coupling reaction that allows installation of quinoxalinones at the C7 position of thiazolino ring-fused 2-pyridones (TRPs) under mild conditions. The methodology tolerates various substituted quinoxalinones and biologically relevant substituents on the C8 position of the TRP. The TRP scaffold has large potential in the development of lead compounds, and while the coupled products are interesting from a drug-development perspective, the methodology will be useful for developing more potent and drug-like TRP-based candidates.
我们开发了一种铱（PPy）光氧化还原催化的交叉偶联反应，该反应能够在温和条件下将喹喔啉酮安装在噻唑啉环稠合的2-吡啶酮（TRP）的C7位置。该方法能够耐受各种取代的喹喔啉酮以及TRP的C8位置上与生物相关的取代基。TRP支架在先导化合物的开发中具有很大潜力，并且从药物开发的角度来看，偶联产物很有趣，该方法将有助于开发更有效且更具药物特性的基于TRP的候选物。
