Visible Light-Promoted Divergent Benzoheterocyclization from Aldehydes for DNA-Encoded Chemical Libraries

作者：Xianfu Fang, Yiting Wang, Pengyang He, Huilin Liao, Gong Zhang, Yangfeng Li, Yizhou Li · 发表于：Organic Letters · 年份：2022 · DOI：10.1021/acs.orglett.2c01187 · 被引用次数：33 · 研究领域：Chemical Synthesis and Analysis、Click Chemistry and Applications、Advanced biosensing and bioanalysis techniques

Benzoheterocyclics have been widely adopted as drug-like core scaffolds that can be incorporated into DNA-encoded chemical library technology for high-throughput hit discovery. Here, we present a visible light-promoted divergent synthesis of on-DNA benzoheterocycles from aldehydes. Four types of DNA-conjugated benzoheterocyclics were obtained under mild conditions with a broad substrate scope. A cross substrate scope study, together with enzymatic ligation and subsequent chemical diversifications, were conducted, demonstrating the feasibility of this approach in DNA-encoded chemical library construction.