A novel Copper‐catalyzed cascade reaction between six‐membered cyclic diaryliodonium salts and nitriles is reported for the facile access to a variety of N‐carbonyl acridanes in good to excellent yields (up to 82%). The reaction is efficient and atom‐economical with a broad substrate scope (e. g. both aryl / alkyl nitriles and substituted / unsubstituted cyclic diaryliodonium salts compatible in the system). This method is particularly useful for the synthesis of substituted N‐carbonyl acridanes which are present in many pharmaceutically important compounds, but are not easy to obtain in conventional approaches. Furthermore, one of the newly synthesized acridanes displayed high antiproliferative activity against MB‐468 cancer cells (IC₅₀=26 nM, comparable to paclitaxel and colchicine) by inhibiting tubulin polymerization. Together, these findings might grant a rapid access to a novel molecular scaffold with potential anticancer utilities.

中文翻译：

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通过一锅铜催化的丁腈与环二苯基碘鎓的双丙烯酸酯化反应合成N-碳酰rid烷作为微管蛋白聚合的强抑制剂

据报道，新颖的铜催化六元环二芳基碘鎓盐与腈之间的级联反应可轻松获得各种N-羰基a啶，收率高达82％。该反应是有效的且原子经济的，具有广泛的底物范围（例如，在系统中相容的芳基/烷基腈和取代/未取代的环状二芳基碘鎓盐）。该方法对于合成取代N-羰基丙烯醛特别有用，取代N-羰基丙烯醛存在于许多重要的药学化合物中，但在常规方法中不易获得。此外，一种新合成的a啶酮对MB‐468癌细胞显示出高抗增殖活性（IC ₅₀通过抑制微管蛋白的聚合，可达到26 nM（与紫杉醇和秋水仙碱相当）。在一起，这些发现可能会允许快速访问具有潜在的抗癌作用的新型分子支架。