DNA-Compatible Huisgen Cycloaddition

In our latest publication, WuXi AppTec scientists introduce two new methods that utilize readily accessible aldehydes to create substituted isoxazolines and isoxazoles by the 1,3-dipolar cycloaddition reaction.

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. 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.