N-Capping of primary amines with 2-acyl-benzaldehydes to give isoindolinones |
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Authors: | Augner Daniel Gerbino Dario C Slavov Nikolay Neudörfl Jörg-Martin Schmalz Hans-Günther |
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Institution: | Department of Chemistry, University of Cologne, Greinstr. 4, 50939 K?ln, Germany. |
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Abstract: | A unique reactivity pattern, first observed in the conversion of the marine natural product pestalone into pestalachloride A, was investigated. It was shown that 2-formyl-arylketones smoothly react with ammonia and primary amines, respectively, under mild conditions to afford 3-substituted isoindolinones in high yield. The reaction represents a new option for the derivatization (N-capping) of primary amines. As the substrates are readily accessible the methodology opens a short and modular access to pharmaceutically relevant substituted isoindolinones. |
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