Pyridine is an essential structural motif in medicinal chemistry and shows a wide range of bioactivities based on its substitution patterns, however, the meta-substitution of pyridine remains challenging. Here, the authors develop the synthesis of dissymmetric di-meta-substituted pyridines from 3-formyl(aza)indoles through the in situ generation of enamines via resonance-assisted hydrogen bonding, showcasing various synthetic applications in medicinal chemistry.
- Sihyeong Yi
- Ji Hyae Lee
- Seung Bum Park
