摘要/Abstract

螺杂环化合物独特的立体结构和丰富的理化特性, 激发了研究工作者对其高效合成方法的持续关注. 炔醇在过渡金属作用下经exo-dig式分子内环化可原位形成环外烯醇醚, 其作为一类高活性的C2合成子, 能够与同时具有亲电和亲核特性的“双亲性底物”发生串联反应, 实现螺杂环骨架的快速构建. 综述了近年来炔醇分子内环化促发的串联反应在螺杂环化合物合成中的应用进展, 以期激发更多相关研究工作的设计与报道. 按照参与螺环构建的“双亲性底物”原子数目的不同进行分类, 重点阐述了反应采用的催化体系和反应机制, 分析了目前该领域存在的挑战, 并对未来的发展进行了展望.
关键词: 螺杂环, 炔醇, 串联反应, 环外烯醇醚
Due to their unique stereoscopic structure and rich physical and chemical properties, spiro heterocyclic compounds have aroused the continuous attention of researchers on their efficient synthesis methods. The exo-cyclic enol ethers generated in situ by exo-dig cyclization of alkynols under the promotion of transition metals could serve as C2 synthons to react with various "amphiphilic substrates" through cascade reactions mode. These cascade reactions could afford spiro heterocyclic skeletons in highly efficient and direct manners. In this paper, the application progress of cascade reactions in the synthesis of sprio-heterocycles initiated by intramolecular cyclization of alkynols is reviewed, which aims to stimulate the disclosure of more related research work. These work is elaborated according to the different atom numbers of the "amphiphilic substrates" involved in the construction of the spiro framworks. The catalytic system and reaction mechanism are mainly described, the challenges in this field are analyzed, and the future development is also put forward.
Key words: sprio-heterocycles, alkynols, cascade reactions, exo-cyclic enol ether


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