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Direct synthesis of 2-oxo-acetamidines from methyl ketones, aromatic amines and DMF via copper-catalyzed C(sp3)–H amidination

机译:通过铜催化的C(sp3)–H酰胺化反应,由甲基酮,芳族胺和DMF直接合成2-氧代乙acet

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A convenient method for the synthesis of 2-oxo-acetamidines from methyl ketones using aromatic amines and DMF as nitrogen sources is reported via copper-catalyzed C(sp ~(3) )–H amidination. Various methyl ketones react readily with aromatic amines and DMF, producing 2-oxo-acetamidines in yields of 47 to 92%. This protocol features the simultaneous formation of C–N and CN bonds using DMF and aromatic amines as two different nitrogen sources. It thus provides an efficient approach to construct acyclic amidines via three C(sp ~(3) )–H bond amidination. Based on the preliminary experiments, a plausible mechanism of this transformation is disclosed.
机译:通过铜催化的C(sp〜(3))–H酰胺化反应,报道了一种使用芳香胺和DMF作为氮源由甲基酮合成2-氧-乙acet的简便方法。各种甲基酮容易与芳族胺和DMF反应,生成2-氧-乙acet,产率为47%至92%。该协议的特征是使用DMF和芳香胺作为两个不同的氮源同时形成C–N和CN键。因此,它提供了一种通过三个C(sp〜(3))-H键酰胺化来构建无环am的有效方法。基于初步实验,揭示了这种转化的合理机制。

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