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目的综述原小檗碱类化合物合成研究的新进展,为开展该类化合物的结构改造提供方法参考。方法依据近十年来国内外文献进行分析、归纳、总结并进行评述。结果与结论原小檗碱类化合物具有广泛的药理活性,其化学结构也有其特殊性,可以看作是由2个异喹啉母核组合构成的4个六元环体系。其中环上氢化程度的改变还会影响整个分子的空间构象,从而影响化合物的药理活性。因此,这类化合物的合成已经成为许多药物化学工作者研究的主要内容之一。其母核的构建研究涵盖传统的异喹啉合成方法及其改进策略,如皮克太特-斯彭格勒反应、毕史勒-那皮拉斯开反应等,以及新颖的C-C键连接方式,如亲核加成环化反应、自由基反应、傅克烷基化反应、钯催化的C-C键偶联反应、环加成反应等。所有这些方法都为我们开展该类化合物的结构改造研究提供了强有力的工具,相信以这些合成方法为基础,该领域的研究者一定能够早日开发出具有新颖结构的原小檗碱类药物先导化合物。
OBJECTIVE To summarize the recent advances in the synthesis of protoberberines and provide references for the structural transformation of these compounds. Methods Based on the domestic and foreign literatures in the past decade, the method is summarized, summarized and reviewed. RESULTS AND CONCLUSION Protoberberines have a wide range of pharmacological activities, and their chemical structure has its own particularity. It can be regarded as four six-membered ring system composed of two isoquinoline mother nuclei. The change of degree of hydrogenation on the ring also affects the spatial conformation of the entire molecule, thereby affecting the pharmacological activity of the compound. Therefore, the synthesis of these compounds has become one of the main contents of many pharmaceutical chemists. The construction of its mother nucleus covers the traditional methods of isoquinoline synthesis and its improvement strategies, such as Pickett-Spentalling reaction, Buchler-Napier opening reaction, as well as the novel CC bond mode , Such as nucleophilic addition cyclization reaction, free radical reaction, Fu Ke alkylation reaction, palladium-catalyzed CC bond coupling reaction, cycloaddition reactions. All of these methods provide a powerful tool for our research on the structural transformation of these compounds. Based on these synthetic methods, researchers in this field will surely be able to pioneer the early development of protoberberines with novel structures Compound.