Ruthenium‐Catalyzed Difluoroalkylation of 8‐Aminoquinoline Amides at the C5‐Position

Abstract

A ruthenium‐catalyzed highly selective difluoromethylation of 8‐aminoquinoline amides at the C5 position has been developed. It tolerates a broad range of functional groups, providing the corresponding difluoromethylated products in moderate to good yields. Preliminary experimental results indicate that the tricoordinate ruthenium intermediate is the key factor in achieving the C5‐position selectivity.