Copper‐Catalyzed C4‐selective Carboxylation of Pyridines with CO2 via Pyridylphosphonium Salts

• DOI: 10.1002/anie.202318572
• Publication Date: 2024-02-03T03:30:25Z
• Authors: Shibiao Tang; Zezhao Liu; Jiakai Zhang; Bin Li; Baiquan Wang
• Keywords: Carboxylation; Surface Modification; Phosphonium

Abstract Pyridine motifs are widespread pharmacophores in many drugs. Installing various substituents through pyridine C−H bond functionalization is significant for new drug design and discovery. Developments of late‐stage reactions enrich the strategies selective pyridines. However, carboxylation pyridines a long‐standing challenge, especially selectively with CO 2 on motifs. Herein, we describe practical method C4−H via one‐pot phosphination copper‐catalyzed resulted phosphonium salts . The reaction conducted under mild conditions compatible multiple active groups several drugs, providing diverse valuable isonicotinic acid compounds, demonstrating application potential this strategy.