Pyridine-Fused 2-Pyridones via Povarov and A 3 Reactions: Rapid Generation of Highly Functionalized Tricyclic Heterocycles Capable of Amyloid Fibril Binding.
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Singh P, Adolfsson DE, Ådén J, Cairns AG, Bartens C, Brännström K, Olofsson A, Almqvist F
J. Org. Chem. 84 (7) 3887-3903 [2019-04-05; online 2019-03-20]
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.
Swedish NMR Centre (SNC) [Service]
PubMed 30862161
DOI 10.1021/acs.joc.8b03015
Crossref 10.1021/acs.joc.8b03015