摘要
杂环化合物包括氮杂环、硫杂环、硅杂环、磷杂环等不同的结构.氮杂环是杂环化合物中最常见和最重要的.Vasicine、Batracylin、Neocryptolepine等活性分子的关键母核均为五元并六元氮杂环骨架,呈现出多样的药理活性.镁、钴、镍等金属是合成氮杂环衍生物常用的催化剂.与前述金属相比,铜具有配体简单、毒性低、条件温和的显著优点,在构建氮杂环骨架中得到了广泛应用.本研究基于铜催化的双环化反应构建五元并六元氮杂环骨架,为探究该类衍生物的合成新法奠定基础.
Abstract
Heterocyclic compounds include nitrogen heterocycles, sulfur heterocycles, silicon heterocycles, phosphorous heterocycles and other different structures. Nitrogen heterocycles are the most common and important heterocyclic compounds. The key nucleus of ac-tive molecules such as Vasicine, Batracylin, Neocryptolepine are all five- and six-membered nitrogen heterocyclic skeletons, showing diverse pharmacological activities. Magnesium, cobalt, nickel and other metals are commonly used catalysts for the synthesis of nitrogen heterocyclics. Compared with the aforementioned metals, copper has the obvious advantages of simple ligands, low toxicity, and mild conditions, which has been widely used in the construction of nitrogen heterocyclic skeletons. This article reports on the construction of a five- and six-membered nitrogen heterocyclic skeleton based on a copper-catalyzed bicyclization reaction, which lays a foundation for exploring new methods for the synthesis of such derivatives.
基金项目
安徽省教育厅自然科学研究重点项目(2023AH052843)
滁州城市职业学院校级平台项目(2023zkzd05)