Allyl-Assisted, Cu(I)-Catalyzed Azide鈥揂lkyne Cycloaddition/Allylation Reaction: Assembly of the [1,2,3]Triazolo-4,5,6,7-tetrahydropyridine Core Structure

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• 作者：Xiaohu Deng ; Jimmy Liang ; Brett B. Allison ; Curt Dvorak ; Heather McAllister ; Brad M. Savall ; Neelakandha S. Mani
• 刊名：Journal of Organic Chemistry
• 出版年：2015
• 出版时间：November 6, 2015
• 年：2015
• 卷：80
• 期：21
• 页码：11003-11012
• 全文大小：654K
• ISSN：1520-6904

文摘

We report a Cu(I)-catalyzed azide鈥揳lkyne鈥揳llyl halide three-component reaction for a one-pot synthesis of 1,4-disubstituted 5-allyl-1,2,3-triazoles. The allyl moiety provides not only the electrophile but also a coordinating ligand to Cu, which is essential for the reaction to occur under mild conditions. A concise synthesis of a potential drug candidate 1 is realized based on this key reaction.