A novel synthesis of N-(piperidin-4-yl)-1,3-dihydroindol-2-one via an intramolecular Pd-catalyzed amination |
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| Authors: | Adri van den Hoogenband Jack AJ den Hartog Jos HM Lange Jan Willem Terpstra |
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| Institution: | Solvay Pharmaceuticals, Research Laboratories, C. J. van Houtenlaan 36, 1381 CP Weesp, The Netherlands |
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| Abstract: | A novel efficient synthetic route to the pharmaceutical key intermediate N-(piperidin-4-yl)-1,3-dihydroindol-2-one is described. The key step involves a high-yielding intramolecular palladium-catalyzed amination reaction using Buchwald’s X-Phos ligand under mild reaction conditions. |
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