Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 22, Issue 7, Pages 2266-2269Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201504823
Keywords
copper; homogeneous catalysis; propargylic amines; synthetic methods; multicomponent reactions
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Funding
- National Natural Science Foundation of China [21232006]
- National Basic Research Program [2015CB856600]
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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.
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