Wang Ming-Yang, Zeng Wei-Long, Chen Lin, Yuan Yu-Fei, Li Wei
Department of Chemistry, Zhejiang University, Hangzhou, 310058, China.
State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin, 300071, China.
Angew Chem Int Ed Engl. 2024 Aug 12;63(33):e202403917. doi: 10.1002/anie.202403917. Epub 2024 Jul 9.
Although dearomative functionalizations enable the direct conversion of flat aromatics into precious three-dimensional architectures, the case for simple arenes remains largely underdeveloped owing to the high aromatic stabilization energy. We herein report a dearomative sequential addition of two nucleophiles to arene π-bonds through umpolung of chromium-arene complexes. This mode enables divergent dearomative carbonylation reactions of benzene derivatives by tolerating various nucleophiles in combination with alcohols or amines under CO-gas-free conditions, thus providing modular access to functionalized esters or amides. The tunable synthesis of 1,3- or 1,4-cyclohexadienes as well as the construction of carbon quaternary centers further highlight the versatility of this dearomatization. Diverse late-stage modifications and derivatizations towards synthetically challenging and bioactive molecules reveal the synthetic utility. A possible mechanism was proposed based on control experiments and intermediate tracking.
尽管去芳构化官能团化能够将平面芳烃直接转化为珍贵的三维结构,但由于芳烃具有较高的稳定化能,简单芳烃的相关研究仍很不充分。我们在此报告了通过铬-芳烃配合物的极性翻转,将两个亲核试剂依次加成到芳烃π键上的去芳构化反应。这种模式能够在无CO气体的条件下,通过与醇类或胺类结合耐受各种亲核试剂,实现苯衍生物的发散性去芳构化羰基化反应,从而提供了一种模块化的方法来合成功能化酯或酰胺。1,3-或1,4-环己二烯的可调合成以及季碳中心的构建进一步突出了这种去芳构化反应的多功能性。针对具有合成挑战性的生物活性分子进行的各种后期修饰和衍生化反应揭示了其合成效用。基于对照实验和中间体跟踪提出了一种可能的机理。