Institute of Organic Chemistry and Center of Biomolecular Drug Research (BMWZ) , Leibniz Universität Hannover , Schneiderberg 1b , Hannover 30167 , Germany.
J Org Chem. 2019 Apr 5;84(7):3887-3903. doi: 10.1021/acs.joc.8b03015. Epub 2019 Mar 20.
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 Aβ and α-synuclein fibrils, which are associated with neurodegenerative diseases.
我们在这里描述了三组分反应在合成三环吡啶环并 2-吡啶酮中的应用。所开发的方法具有广泛的底物范围，并允许在三环中心片段上安装各种化学官能团。这些吡啶稠合的刚性多环化合物中的几种被证明可以结合到与神经退行性疾病相关的 Aβ 和 α-突触核蛋白纤维上。
