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      Metal-Free Oxidative C-H Amidation ofN,N′-Diarylureas with PhI(OAc)2: Synthesis of Benzimidazol-2-one Derivatives : Metal-Free Oxidative C-H Amidation ofN,N′-Diarylureas

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      European Journal of Organic Chemistry
      Wiley

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          The influence of drug-like concepts on decision-making in medicinal chemistry.

          The application of guidelines linked to the concept of drug-likeness, such as the 'rule of five', has gained wide acceptance as an approach to reduce attrition in drug discovery and development. However, despite this acceptance, analysis of recent trends reveals that the physical properties of molecules that are currently being synthesized in leading drug discovery companies differ significantly from those of recently discovered oral drugs and compounds in clinical development. The consequences of the marked increase in lipophilicity--the most important drug-like physical property--include a greater likelihood of lack of selectivity and attrition in drug development. Tackling the threat of compound-related toxicological attrition needs to move to the mainstream of medicinal chemistry decision-making.
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            Biaryl Phosphane Ligands in Palladium-Catalyzed Amination

            Palladium-catalyzed amination reactions of aryl halides have undergone rapid development in the last 12 years, largely driven by the implementation of new classes of ligands. Biaryl phosphanes have proven to provide especially active catalysts in this context. This Review discusses the application of these catalysts in C-N cross-coupling reactions in the synthesis of heterocycles and pharmaceuticals, in materials science, and in natural product synthesis.
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              Copper-mediated coupling reactions and their applications in natural products and designed biomolecules synthesis.

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                Author and article information

                Journal
                European Journal of Organic Chemistry
                Eur. J. Org. Chem.
                Wiley
                1434193X
                September 2015
                September 2015
                July 31 2015
                : 2015
                : 26
                : 5869-5875
                Article
                10.1002/ejoc.201500726
                433d5275-c8aa-495e-9c29-031687a9fe14
                © 2015

                http://doi.wiley.com/10.1002/tdm_license_1.1

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