Rhodium-catalyzed C–H activation and three-component tandem annulation leading to isoquinolones

A rhodium-catalyzed C-H activation and three-component coupling of oxazolines, vinylene carbonate and carboxylic acids has been developed. Various isoquinolone products were constructed under redox-neutral conditions with satisfactory yields. It is worth noting that diverse bioactive carboxylic acids have been proven to be effective substrates, and their application in this protocol has expanded the range of isoquinolones with biologically relevant motifs. Multi-dimensional mechanism exploration experiments and derivatization reactions were studied in sequence to explore the details and application prospects of this transformation. It offers an alternative approach for the synthesis of useful isoquinolone derivatives.