Martin Lang - Applicability Aspects of Transition Metal-Catalyzed Aromatic Amination Protocols in Medicinal Chemistry

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      Publication Details (including relevant citation   information):

      Stefan Tasler, Jan Mies, Martin Lang

      Adv. Synth. Catal. 2007, 349,   2286-300


      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 metalbased protocols   had to be applied for synthesizing structurally diverse compounds   in sufficient amounts (several milligrams) for screening without   any finetuning of conditions and catalytic systems.


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