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Copper-Catalyzed Intramolecular C-H Alkoxylation of Diaryltriazoles: Synthesis of Tricyclic Triazole Benzoxazines. 2020
Xinyuan Ma, and
Haotian Li, and
Hong Xin, and
Weigen Du, and
Edward A Anderson, and
Xian Dong, and
Yubo Jiang
Faculty of Science, Kunming University of Science and Technology, Kunming 650500, China.
An efficient copper-catalyzed intramolecular C-H alkoxylation of 1,4-disubstituted 1,2,3-triazoles has been developed. The chemistry was applied to a wide range of substrates, generating tricyclic benzoxazine-fused 1,2,3-triazoles in good yields. Mechanistic studies suggest that a radical pathway may be involved in this transformation. The triazole products were found to exhibit strong antifungal activity against ginseng root-rot disease, demonstrating their potential as a scaffold in medicinal chemistry research.
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