On-DNA Synthesis of Arylhydrazones via Aryl Diazonium-Mediated Diazenylation

This is the authors' abstract. We don't add key points for this paper.

Arylhydrazones represent a privileged class of scaffolds with diverse biological activities that are widely utilized in medicinal chemistry. Here, we report a mild yet effective strategy for constructing arylhydrazones via the in situ generation of DNA-conjugated aryl diazonium intermediates, followed by subsequent coupling with a variety of active methylene compounds. This method features broad substrate scopes, good to excellent conversions for both DNA-conjugated arylamine and DNA-conjugated active methylene coupling partners, and good compatibility with the DNA-encoded library (DEL) workflow, significantly expanding the accessible chemical space for DEL-based drug discovery.