Synthesis of N-substituted aryl amidines by strong base activation of amines

[Display omitted] We describe an efficient method for the direct preparation of N-substituted aryl amidines from nitriles and primary amines. The protocol employs activation of amines by a strong base and provides greater access to a pharmaceutically relevant functional group. This synthetic approac...

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Veröffentlicht in:Tetrahedron letters 2015-07, Vol.56 (27), p.4109-4111
Hauptverfasser: Khalifa, Muhammad M., Bodner, Micah J., Berglund, J. Andrew, Haley, Michael M.
Format: Artikel
Sprache:eng
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Zusammenfassung:[Display omitted] We describe an efficient method for the direct preparation of N-substituted aryl amidines from nitriles and primary amines. The protocol employs activation of amines by a strong base and provides greater access to a pharmaceutically relevant functional group. This synthetic approach tolerates deactivated nitriles, nitriles with competing substitution sites, and aryl amines.
ISSN:0040-4039
1873-3581
DOI:10.1016/j.tetlet.2015.05.029