Identifying a Highly Active Copper Catalyst for KA2 Reaction of Aromatic Ketones |
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Authors: | Yujuan Cai Dr Xinjun Tang Prof Dr Shengming Ma |
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Institution: | 1. State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai, P. R. China;2. Department of Chemistry, Fudan University, Shanghai, P. R. China |
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Abstract: | The well‐established A3 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 CuI, 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. |
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Keywords: | copper homogeneous catalysis propargylic amines synthetic methods multicomponent reactions |
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