Applicability Aspects of Transition Metal‐Catalyzed Aromatic Amination Protocols in Medicinal Chemistry

Abstract

Abstract The application of palladium‐ and copper‐catalyzed reactions for the aromatic amination of pharmacologically relevant scaffolds is investigated. The focus is set on the scope of several protocols for the introduction of amines of broad structural diversity, allowing for the synthesis of numerous derivatives of one biological hit structure for screening in biological assay systems. Thus, attaining optimized yields and TONs had not a major priority, most important were practical aspects, that is no further purification and drying of reagents and solvents had to be envisaged, ideally only a few transition metal‐based protocols had to be applied for synthesizing structurally diverse compounds in sufficient amounts (several milligrams) for screening without any fine‐tuning of conditions and catalytic systems.