Huanqing Zhang, Yang Chen, Huimin Sun, Li Sang, Lijun Xue, Kexin Yang, Yun Jin Hu
The first mild, on-DNA radical iodosulfonylation of alkynes enables the synthesis of β-iodovinyl sulfones at room temperature while maintaining DNA integrity. This method provides structurally diverse bifunctional intermediates, facilitating late-stage orthogonal functionalization for expanding DNA-encoded library (DEL) chemical space.