Triple‐Bond Directed Csp 2 −N Bond Formation with N ‐Fluorobenzenesulfonimide as Aminating Source: One‐Step Transformation of Aldehydes into Amines

A metal‐free, versatile triple‐bond directed approach for the decarbonylative C−H amination of ortho ‐alkynyl quinoline/pyridine aldehydes using N ‐fluorobenzenesulfonimide as nitrogen source under mild reaction conditions has been described. The designed reaction strategy was triggered by trapping of fluorine by base with subsequent attack of bis(phenylsulfonyl)‐λ 2 ‐azane on the carbonyl carbon of a heterocycle, which was gradually converted into the corresponding amine through a Curtius type rearrangement. This protocol provides a one‐step approach for the conversion of aldehydes into amines in good yields. The synthesized amines were successfully transformed into biologically important pyrroloquinolines/pyridines.