Direct C4–H amination of pyridines and quinolines under benign conditions
Abstract
position, followed by subsequent conversion to the amine functionality-a process that suffers from low atom economy and generates substantial waste. Herein, we report a straightforward and environmentally benign method for the direct C4-H amination of azines. This transition-metal-free protocol, employing a base and an activating agent in ethyl acetate, enables mild and efficient C4-H amination of a wide range of 2-substituted pyridines and quinolines. Furthermore, we demonstrate that regioselectivity is strongly influenced by both substrate structure and solvent, and provide practical guidelines for optimal substrate selection.
Fields of Study & Subjects
Synthesis and Catalytic Reactions
Catalytic C–H Functionalization Methods
Catalytic Cross-Coupling Reactions
Publication details
- Journal / source
- Organic & Biomolecular Chemistry
- Publisher
- Royal Society of Chemistry (RSC)
- Volume
- 24
- Issue
- 25
- Pages
- 5308–5317
- Publication date
- 1 January 2026
- Language
- EN