title: Enantioselective Synthesis of 3-Alkynyl-3-hydroxyindolin-2-ones by Copper-Catalyzed Asymmetric Addition of Terminal Alkynes to Isatins.
abstract: A highly efficient copper-catalyzed asymmetric addition of terminal alkynes to isatins has been developed. In the presence of a catalytic amount of copper iodide and a chiral phosphine ligand, the reaction gave the corresponding chiral 3-alkynyl-3-hydroxyindolin-2-ones in high yields with high enantioselectivity. This methodology has a broad substrate scope, and the synthetic utility of the present protocol was further demonstrated by the transformation of chiral alkynylation products.
authors.affiliation: Key Laboratory for Advanced Materials and Institute of Fine Chemicals, East China University of Science and Technology , Shanghai 200237, P. R. China.
authors.forename: Ning
authors.initials: N
authors.lastname: Xu
authors.affiliation: Shanghai Center for Systems Biomedicine, Ministry of Education Key Laboratory of Systems Biomedicine, Shanghai Jiao Tong University , Shanghai 200240, P. R. China.
authors.forename: Da-Wei
authors.initials: DW
authors.lastname: Gu
authors.affiliation: Shanghai Center for Systems Biomedicine, Ministry of Education Key Laboratory of Systems Biomedicine, Shanghai Jiao Tong University , Shanghai 200240, P. R. China.
authors.forename: Jing
authors.initials: J
authors.lastname: Zi
authors.affiliation: Key Laboratory for Advanced Materials and Institute of Fine Chemicals, East China University of Science and Technology , Shanghai 200237, P. R. China.
authors.forename: Xin-Yan
authors.initials: XY
authors.lastname: Wu
authors.affiliation: Shanghai Center for Systems Biomedicine, Ministry of Education Key Laboratory of Systems Biomedicine, Shanghai Jiao Tong University , Shanghai 200240, P. R. China.|State Key Laboratory of Elemento-organic Chemistry, Nankai University , Tianjin 300071, P. R. China.
authors.forename: Xun-Xiang
authors.initials: XX
authors.lastname: Guo