Xianfeng Li; Changyang Liu; Yuting Gao; Gong Zhang; Yangfeng Li; Yizhou Li
Chem. Commun., 2023, 59, 9489-9492
https://doi.org/10.1039/D3CC02593D

Abstract

2-Thiobenzazole is among the privileged heterocyclic scaffolds in medicinal chemistry. Constructing such structural components in DNA-encoded libraries (DELs) may promote related bioactive hit discovery in a high-throughput fashion. Herein, we reported a DNA-compatible mild-condition synthetic methodology to efficiently forge functionalized 2-thiobenzazole scaffolds, realizing on-DNA sulfhydryl incorporation with broad substrate scope, thereby expanding the scope of 2-thiobenzazole-focused DNA-encoded chemical libraries.