title: Identifying a Highly Active Copper Catalyst for KA(2) Reaction of Aromatic Ketones.
abstract: The well-established A(3) coupling reaction of terminal alkynes, aldehydes, and amines provides the most straightforward approach to propargylic amines. However, the related reaction of ketones, especially aromatic ketones, is still a significant challenge. A highly efficient catalytic protocol has been developed for the coupling of aromatic ketones with amines and terminal alkynes, in which Cu(I) , generated in situ from the reduction of CuBr2 with sodium ascorbate, has been identified as the highly efficient catalyst. Since propargylic amines are versatile synthetic intermediates and important units in pharmaceutical products, such an advance will greatly stimulate research interest involving the previously unavailable propargylic amines.
authors.affiliation: State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Lu, Shanghai, 200032, P. R. China.
authors.forename: Yujuan
authors.initials: Y
authors.lastname: Cai
authors.affiliation: State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Lu, Shanghai, 200032, P. R. China.
authors.forename: Xinjun
authors.initials: X
authors.lastname: Tang
authors.affiliation: State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Lu, Shanghai, 200032, P. R. China. masm@sioc.ac.cn.|Department of Chemistry, Fudan University, 220 Handan Road, Shanghai, 200433, P. R. China. masm@sioc.ac.cn.
authors.forename: Shengming
authors.initials: S
authors.lastname: Ma
keywords: copper; homogeneous catalysis; multicomponent reactions; propargylic amines; synthetic methods