Xianfu Fang; Yiting Wang; Pengyang He; Huilin Liao; Gong Zhang; Yangfeng Li; Yizhou Li
Org. Lett., 2022, 24(17), 3291-3296
https://doi.org/10.1021/acs.orglett.2c01187

Abstract

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.