Rh(III)-Catalyzed Intermolecular C–H Amination of 1‑Aryl‑1<i>H</i>‑pyrazol-5(4<i>H</i>)‑ones with Alkylamines

Abstract

An intermolecular C–H amination of 1-aryl-1<i>H</i>-pyrazol-5­(4<i>H</i>)-ones was achieved under mild reaction conditions, using a low catalyst loading and with a broad scope of aminating reagents. This protocol not only provides the first example of rhodium­(III)-catalyzed intermolecular aromatic C–H amination directed by an intrinsic functionality of the substrate/product but also features aminating an existing drug with either primary or secondary <i>N</i>-benzoate alkylamines as the coupling partners