Yue Ji; Dongliang Dai; Huadong Luo; Simin Shen; Jing Fan; Zhao Wang; Min Chen; Jinqiao Wan; Jin Li; Huiyong Ma; Guansai Liu
Bioconjugate Chem., 2021, 32(4), 685–689
https://doi.org/10.1021/acs.bioconjchem.1c00076

Abstract

Thioethers have been widely found in biologically active compounds, including pharmaceuticals. In this report, a highly efficient approach to on-DNA construction of thioethers via Cu-promoted Ullmann cross-coupling between DNA-conjugated aryl iodides and thiols is developed. This methodology was demonstrated with medium to high yields, without obvious DNA damage. This reported reaction has strong potential for application in DNA-encoded chemical library synthesis.