烯酮的直接区域选择性γ-胺化反应
Direct Regioselective γ-Amination of Enones.
作者信息
Chen Xiaohong, Liu Xiaoguang, Mohr Justin T
机构信息
Department of Chemistry, University of Illinois at Chicago , 845 West Taylor Street, Chicago, Illinois 60607, United States.
出版信息
Org Lett. 2016 Feb 19;18(4):716-9. doi: 10.1021/acs.orglett.5b03689. Epub 2016 Feb 3.
PMID:26840753
Abstract
Carbonyl compounds bearing a γ-amino group are valuable pharmacologically active targets. Regioselective γ-C-N bond formation is achieved with simple enone substrates through controlled dienolate reactivity toward azodicarboxylate electrophiles. The amination reaction occurs readily with sterically demanding nucleophiles and is stereoselective.
摘要
带有γ-氨基的羰基化合物是有价值的药理活性靶点。通过控制烯醇酸酯对偶氮二甲酸酯亲电试剂的反应性，利用简单的烯酮底物实现区域选择性γ-C-N键的形成。胺化反应很容易与空间位阻较大的亲核试剂发生，并且具有立体选择性。
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