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

被引:15
|
作者
Khalifa, Muhammad M. [1 ]
Bodner, Micah J. [1 ]
Berglund, J. Andrew [1 ,2 ]
Haley, Michael M. [1 ]
机构
[1] Univ Oregon, Dept Chem & Biochem, Eugene, OR 97403 USA
[2] Univ Oregon, Inst Mol Biol, Eugene, OR 97403 USA
基金
美国国家卫生研究院;
关键词
Amidine; Amine; Nitrile; Base-activation; Strong base; ANTIPROTOZOAL ACTIVITY; MYOTONIC-DYSTROPHY; DERIVATIVES; PENTAMIDINE; BINDING; NITRILES; ANALOGS; AGENTS; INHIBITOR; MOLECULES;
D O I
10.1016/j.tetlet.2015.05.029
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
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.
引用
收藏
页码:4109 / 4111
页数:3
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