Rhodium-Promoted C-H Activation/ Annulation between DNA-Linked Terminal Alkyne and Aromatic Acid: A Finding from the Selection Outcomes

As discovered by the previous selection outcomes, we developed a Rhodium-promoted C-H activation/ annulation reaction of DNA-linked terminal alkyne and aromatic acid. This reaction exhibits excellent efficiency with high conversions and a wide broad sub-strate scope. Most importantly, the unique DEL-compatible condition provides a better scenario to yield an isocoumarin scaffold compared to conventional organic reaction condition, and this newly developed on-DNA method has confirmed its feasibility in preparing DNA-encoded libraries.