Pyridine-Fused 2-Pyridones via Povarov and A3 Reactions: Rapid Generation of Highly Functionalized Tricyclic Heterocycles Capable of Amyloid Fibril Binding
Pyridine-Fused 2-Pyridones via Povarov and A3 Reactions: Rapid Generation of Highly Functionalized Tricyclic Heterocycles Capable of Amyloid Fibril Binding
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DOI：
10.1021/acs.joc.8b03015
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发表时间：
2019-04-05
影响因子：
3.6
通讯作者：
Almqvist, Fredrik
中科院分区：
文献类型：
--
作者：
Singh, Pardeep;Adolfsson, Dan E.;Almqvist, Fredrik
本文介绍了用三组分反应合成三环吡啶- 2-吡啶酮的方法。开发的协议具有广泛的底物范围，并允许在三环中心片段上安装不同的化学功能。其中一些吡啶融合的刚性多杂环被证明与Afi和a-突触核蛋白原纤维结合，这与神经退行性疾病有关。
We here describe the use of three-component reactions to synthesize tricyclic pyridine ring-fused 2-pyridones. The developed protocols have a wide substrate scope and allow for the installation of diverse chemical functionalities on the tricyclic central fragment. Several of these pyridine-fused rigid polyheterocycles are shown to bind to Afi and a-synuclein fibrils, which are associated with neurodegenerative diseases.