Work

Dual Ligand‐Enabled Nondirected C─H Olefination of (Hetero)Arenes for the Synthesis of Clickable Derivatives

Year: 2026

Type: article

Abstract: Herein, we present a highly efficient method for the late-stage introduction of "clickable" alkyne moieties into different (hetero)arene scaffolds. A highly efficient dual ligand-based palladium catalyst combining an N-acylsulfonamide (NASA) ligand with an N-heterocycle enables the introduction of acrylate moiety bearing a terminal alkyne via nondirected C─H activation, providing a versatile platform for subsequent bioconjugation or activity-based protein profiling (ABPP) applications. The utility of the method is demonstrated through a broad substrate scope and the subsequent use of the obtained products in representative click reactions.

Source: Chemistry - A European Journal

DOI: 10.1002/chem.202600018

Authors: Tommaso Braga, Maria Hergert, Manuel van Gemmeren

Institution: Christian-Albrechts-Universität zu Kiel

Language: English

Topic: Catalytic C–H Functionalization Methods

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

Open Access status: hybrid

Estimated APC paid: $4,640

Funders: European Commission, European Research Council