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目的:为了使小檗碱能与一定的化学成分拼接,很大程度上需要形成一个中间体。通过设计与实验,合成出9-O氨基小檗碱衍生物。方法:以小檗碱为起始物,通过去甲基、溴代、氨基化等反应,先后制得小檗红碱,9-O-(4’-溴丁烷)小檗碱,最终合成9-O-(4’-胺丁基)小檗碱,并通过波谱手段确定其相对分子质量和分子结构。结果:通过一系列化学反应有机合成成功制得小檗红碱与9-O-(4’-溴丁烷)小檗碱,通过对文献方法的综合、优化制备出9-O-(4’-胺丁基)小檗碱衍生物,并通过ESI-MS、核磁谱确定了其相对分子质量、分子式以及分子结构。结论:通过对方法的优化,大大提高了产物9-O-(4’-胺丁基)小檗碱的得率,并且合成过程简便易操作。从目标物结构来看,端基为氨基,是活泼的基团,可与多种化学基团进行反应,进而引入新的基团,合成得到更多衍生物。
Objective: In order to berberine can be spliced with a certain chemical composition, to a large extent, need to form an intermediate. Through the design and experiment, synthetic 9-O amino berberine derivatives. Methods: Berberine was used as the starting material to prepare berberine and 9-O- (4’-bromobutane) berberine through demethylation, bromination, 9-O- (4’-aminebutyl) berberine, and its relative molecular mass and molecular structure were determined by spectroscopic methods. Results: Berberine and 9-O- (4’-bromobutane) berberine were successfully synthesized through a series of chemical reactions. The synthesis of 9-O- (4’- - aminebutyl) berberine derivatives, and its relative molecular mass, molecular formula and molecular structure were confirmed by ESI-MS and NMR. Conclusion: The yield of 9-O- (4’-aminebutyl) berberine is greatly improved by the optimization of the method, and the synthesis process is simple and easy to operate. From the target structure point of view, the terminal group is amino, is a lively group, with a variety of chemical groups to react, and then introduce new groups, more derivatives were synthesized.