Abstract：
A facile and novel synthetic method for the synthesis of functionalized polycyclic coumarins at the C-4 and C-5 positions is proposed for the first time, which employs copper-catalyzed addition reactions of undiscovered alkenes with difluoromethyl radicals to construct polycyclic coumarins. This strategy is characterized by high regioselectivity, easy availability of raw materials, and simple operation. Additionally, such undiscovered coumarin alkenes can be reacted with a variety of difluoromethyl precursors to obtain a wide range of valuable C-4 and C-5 position functionalized/difluoromethylated polycyclic coumarins. More importantly, some of the products showed significant inhibition of proliferation in vitro against melanoma B16-F10 and lung cancer A549 cell lines with optimal IC50 values of 8.57 and 16.04 μM, respectively.
摘要：
首次提出了一种在C-4和C-5位合成官能化多环香豆素的简便而新颖的合成方法，它利用铜催化的未发现的烯烃与二氟甲基自由基的加成反应来构建多环香豆素。这种策略的特点是高区域选择性，原材料容易获得，操作简单。此外,这种未发现的香豆素烯烃可以与多种二氟甲基前体反应以获得宽范围的有价值的C-4和C-5位官能化/二氟甲基化多环香豆素。更重要的是,某些产品在体外对黑色素瘤B16-F10和肺癌A549细胞系的增殖具有显着的抑制作用，最佳IC50值为8.57和16.04μM，分别。
