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

TETRAHEDRON LETTERS

卷:56

Article

Khalifa, Muhammad M.¹  Bodner, Micah J.¹  Berglund, J. Andrew^1,2  Haley, Michael M.¹ 

[1] Univ Oregon, Dept Chem & Biochem, Eugene, OR 97403 USA

[2] Univ Oregon, Inst Mol Biol, Eugene, OR 97403 USA

关键词: Amidine;    Amine;    Nitrile;    Base-activation;    Strong base;   

DOI  :  10.1016/j.tetlet.2015.05.029

来源: Elsevier

【 摘 要 】

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. (C) 2015 Elsevier Ltd. All rights reserved.

【 授权许可】

Free