Department of Chemistry and Biochemistry and School of Green Chemistry and Engineering, The University of Toledo, Toledo, Ohio 43606, USA.
Org Biomol Chem. 2019 Feb 13;17(7):1643-1654. doi: 10.1039/c8ob02443j.
Saturated heterocycles are important structural motifs in a range of pharmaceuticals and agrochemicals. As a result of their importance, syntheses of these molecules have been extensively investigated. Despite the progress in this area, the most adopted strategies are still often characterized with inefficiency or relying on functionalizations with specialized precursors and pre-existing cores. This review highlights a dynamic synthetic strategy for the direct synthesis of saturated heterocycles from intermolecular alkene difunctionalizations. These coupling processes are highly modular, and therefore, offer perhaps the most convenient means to prepare diverse heterocyclic structures in compound libraries for bioactivity evoluations.
饱和杂环是一系列药物和农用化学品的重要结构基序。由于其重要性，这些分子的合成已得到广泛研究。尽管在这一领域取得了进展，但最常用的策略仍然往往效率低下，或者依赖于专门的前体和预先存在的核的官能化。本文综述了一种从分子间烯烃双官能化直接合成饱和杂环的动态合成策略。这些偶联过程具有高度的模块化，因此为在化合物库中进行生物活性进化提供了制备各种杂环结构的最便捷手段。
