title: Allyl-Assisted, Cu(I)-Catalyzed Azide-Alkyne Cycloaddition/Allylation Reaction: Assembly of the [1,2,3]Triazolo-4,5,6,7-tetrahydropyridine Core Structure.
abstract: 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.
authors.affiliation: Janssen Research & Development LLC , 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Xiaohu
authors.initials: X
authors.lastname: Deng
authors.affiliation: Janssen Research & Development LLC , 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Jimmy
authors.initials: J
authors.lastname: Liang
authors.affiliation: Janssen Research & Development LLC , 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Brett B
authors.initials: BB
authors.lastname: Allison
authors.affiliation: Janssen Research & Development LLC , 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Curt
authors.initials: C
authors.lastname: Dvorak
authors.affiliation: Janssen Research & Development LLC , 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Heather
authors.initials: H
authors.lastname: McAllister
authors.affiliation: Janssen Research & Development LLC , 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Brad M
authors.initials: BM
authors.lastname: Savall
authors.affiliation: Janssen Research & Development LLC , 3210 Merryfield Row, San Diego, California 92121, United States.
authors.forename: Neelakandha S
authors.initials: NS
authors.lastname: Mani