Site‐Selective 1,4‐Difunctionalization of Nitrogen Heteroaromatics for Constructing Vinylidene Heterocycles

Abstract A one‐pot protocol for constructing 1,4‐difunctionalized quinoline/pyridine derivatives via the reaction of N‐heteroaromatics, alkyl halides, and active methylene/methyl compounds was developed. The transformation involves dearomative functionalization of an in situ‐activated N‐heteroaromatic to construct new C−N and C=C bonds. This reaction has a broad substrate scope and functional group tolerance. magnified image