Allyl-Assisted, Cu(I)-Catalyzed Azide–Alkyne Cycloaddition/Allylation Reaction: Assembly of the [1,2,3]Triazolo-4,5,6,7-tetrahydropyridine Core Structure
作者:Xiaohu Deng、Jimmy Liang、Brett B. Allison、Curt Dvorak、Heather McAllister、Brad M. Savall、Neelakandha S. Mani
DOI:10.1021/acs.joc.5b02174
日期:2015.11.6
We report a Cu(I)-catalyzed azide-alkyne-allyl 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.