Yuhan Lv; Min Wu; Weiwei Lu; Meiying Cui; Jiaxiang Liu; Wei Yi; Xuan Wang; Xiaojie Lu
Org. Lett., 2024, XXXX, XXX, XXX-XXX
https://doi.org/10.1021/acs.orglett.4c01553

Abstract

Inspired by previous selection outcomes, we investigated and developed a rhodium-promoted C-H activation/annulation reaction of DNA-linked terminal alkynes and aromatic acids. This reaction exhibits excellent efficiency with high conversions and a broad substrate scope. Most importantly, the unique DEL-compatible conditions provide a better scenario for yielding an isocoumarin scaffold compared to conventional organic reaction conditions, and this newly developed on-DNA method has confirmed its feasibility in preparing DNA-encoded libraries.