- Electrochemical C-H Halogenations of Enaminones and Electron-Rich Arenes with Sodium Halide (NaX) as Halogen Source for the Synthesis of 3-Halochromones and Haloarenes
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Without employing an external oxidant, the simple synthesis of 3-halochromones and various halogenated electron-rich arenes has been realized with electrode oxidation by employing the simplest sodium halide (NaX, X = Cl, Br, I) as halogen source. This electrochemical method is advantageous for the simple and mild room temperature operation, environmental friendliness as well as broad substrate scope in both C-H bond donor and halogen source components.
- Lin, Yan,Jin, Jun,Wang, Chaoli,Wan, Jie-Ping,Liu, Yunyun
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p. 12378 - 12385
(2021/09/07)
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- Synthesis of 3-halochromones with simple KX halogen sources enabled by: In situ halide oxidation
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On the basis of a designated in situ oxidation tactic, the synthesis of 3-halochromones has been realized for the first time by using simple KX (X = Br, I) salts as halogen sources. Instead of the free radical process, the control experiments indicate that the reported reactions proceed through a halogenium intermediate. Compared to the known synthetic methods relying on molecular halogen, haloid acid or N-halosuccinimide as the halogen source, the present method is attractive due to its higher atom economy and being more friendly to the operator, thus providing a practical complimentary approach to the preparation of useful halochromone compounds.
- Lin, Yan,Liu, Yunyun,Wan, Jie-Ping
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p. 8120 - 8124
(2020/06/09)
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- Chromenones as potent bradykinin B1 antagonists
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A series of fused 6,6-bicyclic chromenones was investigated for activity against the bradykinin B1 receptor. SAR studies based on a pharmacophore model revealed compounds with high affinity for both human and rabbit B1. These compounds demonstrated favorable pharmacokinetic properties and 5-chlorochromenone 15 was efficacious in a carrageenan-induced mechanical hyperalgesia model for chronic pain.
- Bryan, Marian C.,Biswas, Kaustav,Peterkin, Tanya A.N.,Rzasa, Robert M.,Arik, Leyla,Lehto, Sonya G.,Sun, Hong,Hsieh, Feng-Yin,Xu, Cen,Fremeau, Robert T.,Allen, Jennifer R.
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scheme or table
p. 619 - 622
(2012/02/04)
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