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

ABSTRACT: 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.

SUBMITTER: Khalifa MM

PROVIDER: S-EPMC4470429 | biostudies-literature | 2015 Jul

REPOSITORIES: biostudies-literature

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

Khalifa Muhammad M MM Bodner Micah J MJ Berglund J Andrew JA Haley Michael M MM

Tetrahedron letters 20150701 27

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. ...[more]

PMID: 26097266

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