Herein, we describe a copper photoredox catalyzed synthesis of acetamide via regioselective C–N coupling of arylamines with terminal alkynes using molecular oxygen (O₂) as an oxidant at room temperature under visible light irradiation (47 examples). Unique simultaneous formation of both amide and ester functionalities occurs via intramolecular cyclization in a single-step reaction in the case of anthranilic acids using inexpensive copper as a catalyst and eco-friendly O₂ as an oxidant and reagent. Different substrates undergo different reaction pathways to generate similar acetamide products, as evidenced by ¹⁸O₂ labelling experiments. The current protocol was also applied for the rapid, few step preparation of biologically active inhibitors (BACE-1 and PDE4). This process can be readily scaled up to a gram scale, and calculations of green metrics suggest the economic feasibility and eco-friendly nature of the current photoredox approach.

中文翻译：

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可见光促进的铜催化芳基胺对末端炔烃的区域选择性乙酰胺化

本文中，我们描述了在室温下在可见光照射下，使用分子氧（O ₂）作为氧化剂，通过芳基胺与末端炔烃的区域选择性C–N偶联，通过铜的光氧化还原催化乙酰胺的合成（47个例子）。在邻氨基苯甲酸的情况下，使用便宜的铜作为催化剂，使用环保的O ₂作为氧化剂和试剂，通过一步一步反应通过分子内环化，可以同时形成酰胺和酯官能团。¹⁸ O ₂证明，不同的底物经历不同的反应途径以生成相似的乙酰胺产物。标记实验。当前的方案也适用于快速，少步制备生物活性抑制剂（BACE-1和PDE4）。这个过程可以很容易地放大到克级，绿色度量的计算表明了当前光氧化还原方法的经济可行性和生态友好性。