Catalytic Arylation of a CH Bond in Pyridine and Related Six-Membered N-Heteroarenes Using Organozinc Reagents

Despite significant advances in the catalytic direct arylation of heteroarenes, the application of this reaction to pyridines has been met with limited success. An oxidative nucleophilic arylation strategy has been developed to overcome this problem. Pyridine, pyrazine, quinolone, and related electron‐deficient N‐heteroarenes can be arylated at the most electrophilic site using the developed nickel‐catalyzed reaction. This protocol serves as a complementary method to catalytic direct arylation reactions. Less is more: Pyridine, pyrazine, quinoline and related electron‐deficient N‐heteroarenes can be arylated at the most electrophilic site using organozinc reagents through nickel catalysis. This protocol serves as a complementary method to catalytic direct arylation reactions.