DNA-Compatible Huisgen [3 + 2] Cycloaddition of In Situ Formed Nitrile Oxides with Alkenes or Alkynes to Synthesize Isoxazolines or Isoxazoles

Isoxazoles and isoxazolines, known for their diverse bioactivities—including antibacterial, antifungal, and insecticidal properties—are now accessible through a novel DNA-compatible method developed in this study and published in The Journal of Organic Chemistry. This approach enables the in situ formation of these heterocyclic cores and their efficient incorporation into DNA-encoded libraries (DELs). With high functional group selectivity and a broad substrate scope, the method facilitates the synthesis and exploration of diverse isoxazole and isoxazoline analogues, advancing the development of novel bioactive compounds in drug discovery.

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