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Identifying a Highly Active Copper Catalyst for KA(2) Reaction of Aromatic Ketones

机译:确定高活性铜催化剂的芳香酮的KA(2)反应

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摘要

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.
机译:末端炔烃,醛和胺的公认的A(3)偶联反应为炔丙基胺提供了最直接的方法。然而,酮,特别是芳族酮的相关反应仍然是一个重大挑战。已经开发了用于芳族酮与胺和末端炔烃的偶联的高效催化方案,其中已将通过用抗坏血酸钠还原CuBr 2原位生成的Cu-1确定为高效催化剂。由于炔丙基胺是通用的合成中间体和医药产品中的重要单元,因此这种进展将极大地激发人们对以前不可用的炔丙基胺的研究兴趣。

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