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首页> 外文期刊>RSC Advances >A one pot protocol to convert nitro-arenes into N-aryl amides
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A one pot protocol to convert nitro-arenes into N-aryl amides

机译：将硝基芳烃转化为N-芳基酰胺的一种罐方案

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A two-step one pot, experimentally simple protocol, based on readily available and inexpensive reagents allowed the conversion of nitro-arenes directly to N -aryl amides. A metal-free reduction of the nitro group, mediated by trichlorosilane, followed by the addition of an anhydride afforded the corresponding N -aryl carboxyamide, that was isolated after a simple aqueous work up in good-excellent yields. When the methodology was applied to the reaction with γ-butyrolactone, the desired N -aryl butanamide derivative was obtained, featuring a chlorine atom at the γ-position, a functionalized handle that can be used for further synthetic manipulation of the reaction product. Such an intermediate has already been employed as a key advanced precursor of pharmaceutically active compounds.
机译：基于容易获得和廉价的试剂的两步一锅，实验简单的协议允许直接转化硝基芳烃至N-亚芳酰胺。由三氯硅烷介导的硝基的无金属减少，然后加入酸酐得到相应的N-芳基羧酰胺，其在一个简单的水性余量以优质的产率下分离。当方法与γ-丁内酯的反应应用时，获得所需的N-芳基丁酰胺衍生物，以γ-位置处具有氯原子，该官能化手柄可用于进一步的反应产物的合成操纵。已经使用这种中间体作为药物活性化合物的关键晚期前体。

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