DOI: 10.1021/acs.orglett.6c03236 ISSN: 1523-7060
On-DNA Radical Iodosulfonylation of Alkynes: Access to Bifunctional Covalent Warheads and Modular Scaffolds
Huanqing Zhang, Yang Chen, Huimin Sun, Li Sang, Lijun Xue, Kexin Yang, Yun Jin HuAbstract
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.