- Synthesis and Quantitative Structure-Activity Relationships of Dequalinium Analogues as K+ Channel Blockers: Investigation into the Role of the Substituent at Position 4 of the Quinoline Ring
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Dequalinium (4) is a potent and selective blocker of small conductance Ca2+-activated K+ channels, an important but relatively little studied class.The 4-NH2 group of dequalinium has been shown to contribute significantly to blocking
- Galanakis, Dimitrios,Calder, Julie A. D.,Ganellin, C. Robin,Owen, Clive S.,Dunn, Philip M.
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- Metal-free, redox-neutral, site-selective access to heteroarylamine via direct radical?radical cross-coupling powered by visible light photocatalysis
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Transition-metal-catalyzed C?N bond-forming reactions have emerged as fundamental and powerful tools to construct arylamines, a common structure found in drug agents, natural products, and fine chemicals. Reported herein is an alternative access to heteroarylamine via radical?radical cross-coupling pathway, powered by visible light catalysis without any aid of external oxidant and reductant. Only by visible light irradiation of a photocatalyst, such as a metal-free photocatalyst, does the cascade single-electron transfer event for amines and heteroaryl nitriles occur, demonstrated by steady-state and transient spectroscopic studies, resulting in an amine radical cation and aryl radical anion in situ for C?N bond formation. The metal-free and redox economic nature, high efficiency, and site-selectivity of C?N cross-coupling of a range of available amines, hydroxylamines, and hydrazines with heteroaryl nitriles make this protocol promising in both academic and industrial settings.
- Zhou, Chao,Lei, Tao,Wei, Xiang-Zhu,Ye, Chen,Liu, Zan,Chen, Bin,Tung, Chen-Ho,Wu, Li-Zhu
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supporting information
p. 16805 - 16813
(2020/11/09)
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- Lewis acid activation of pyridines for nucleophilic aromatic substitution and conjugate addition
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A clean, mild and sustainable method for the functionalization of pyridines and their analogues is reported. A zinc-based Lewis acid is used to activate pyridine and its analogues towards nucleophilic aromatic substitution, conjugate addition, and cyclization reactions by binding to the nitrogen on the pyridine ring and activating the pyridine ring core towards further functionalization.
- Abou-Shehada, Sarah,Teasdale, Matthew C.,Bull, Steven D.,Wade, Charles E.,Williams, Jonathan M. J.
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p. 1083 - 1087
(2015/03/30)
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