Maksym V Herasymchuk, Kostiantyn P Melnykov, Tetiana V Druzhenko, Yaroslav I Filatov, Dmytro V Dudenko, Eugeniy M Ostapchuk, Dmytro M Volochnyuk, Serhiy V Ryabukhin
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引用次数: 0
Abstract
Through this model study, we showed broad perspectives on utilizing the diversity-oriented synthesis (DOS) like approach on the building block level in combination with well-developed methodologies for parallel synthesis for decoration and extension of ultra-large tangible chemical space to increase the speed and quality of drug discovery screening campaigns. This strategy led us to 16 novel Bemis-Murco scaffolds based on spirocyclic functionalized piperidines. The efficient, preparative, and scalable DOS-like approach to the above-mentioned motif was achieved by Petasis/Grubbs reactions sequence on a multigram scale. The chemoinformatically generated amide-based compound libraries demonstrated significant expansion of the chemical space of tangible compounds (on the example of Enamine's REAL database).
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Chemistry—A European Journal is a truly international journal with top quality contributions (2018 ISI Impact Factor: 5.16). It publishes a wide range of outstanding Reviews, Minireviews, Concepts, Full Papers, and Communications from all areas of chemistry and related fields.
Based in Europe Chemistry—A European Journal provides an excellent platform for increasing the visibility of European chemistry as well as for featuring the best research from authors from around the world.
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Chemistry—A European Journal is published on behalf of ChemPubSoc Europe, a group of 16 national chemical societies from within Europe, and supported by the Asian Chemical Editorial Societies. The ChemPubSoc Europe family comprises: Angewandte Chemie, Chemistry—A European Journal, European Journal of Organic Chemistry, European Journal of Inorganic Chemistry, ChemPhysChem, ChemBioChem, ChemMedChem, ChemCatChem, ChemSusChem, ChemPlusChem, ChemElectroChem, and ChemistryOpen.
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