作者:Elisabetta Massolo、Margherita Pirola、Alessandra Puglisi、Sergio Rossi、Maurizio Benaglia
DOI:10.1039/c9ra10758d
日期:——
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
基于容易获得且廉价的试剂的两步一锅、实验简单的方案允许将硝基芳烃直接转化为N-芳基酰胺。由三氯硅烷介导的硝基的无金属还原,然后添加酸酐,得到相应的N-芳基羧酰胺,在简单的水处理后以良好的产率分离。当该方法应用于与γ-丁内酯的反应时,获得了所需的N-芳基丁酰胺衍生物,其特征在于γ位上有一个氯原子,这是一个功能化的手柄,可用于进一步合成操作反应产物。这种中间体已被用作药物活性化合物的关键先进前体。