Palladium‐Catalyzed Heck‐Type Double Arylation of 1,2‐Dihydropyridines

ABSTRACT

We report a site‐ and regioselective Heck‐type double arylation of substituted 1,2‐dihydropyridines. This transformation provides access to 2‐substituted 3,6‐diarylated 1,2‐dihydropyridines from readily available dearomatized pyridine derivatives. Two complementary strategies were developed: a direct double arylation approach that rapidly furnishes symmetrically diarylated products and a sequential arylation strategy that enables the controlled introduction of two different aryl groups. Both approaches proceed with generally high selectivity and tolerate different 1,2‐dihydropyridine substrates and aryl iodides. Overall, this study provides a concise entry to highly substituted 1,2‐dihydropyridine scaffolds.