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

Xianfu Fang, Yiting Wang, Pengyang He, Huilin Liao, Gong Zhang, Yangfeng Li, Yizhou Li

Organic letters 2022 May 06

filter terms:

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.

Citation

Xianfu Fang, Yiting Wang, Pengyang He, Huilin Liao, Gong Zhang, Yangfeng Li, Yizhou Li. Visible Light-Promoted Divergent Benzoheterocyclization from Aldehydes for DNA-Encoded Chemical Libraries. Organic letters. 2022 May 06;24(17):3291-3296