由黄连总碱生成四羟基四氢小檗原碱的工艺研究

Synthesis of Tetrahydroberberine from Rhizoma Coptidis

主要探讨从植物黄连中制取标题化合物的生产工艺,并以其为中间体,经甲基化制得四氢巴马汀。首先用酸水浸渍法提取黄连总碱,用硼氢化钠加氢还原,然后加入路易斯酸进行脱甲基和亚甲基,从而制得标题化合物。再以甲苯作溶剂,加入一定量的碘甲烷,从而合成四氢巴马汀。结果表明,合成方法可行,并且可以利用标题化合物为母体合成四氢巴马汀,证明研究的正确性。

The production process of tetrahydroberberine from plants in the production of coptis chinensis is followed. Firstly, using a sulphuric acid solution to extract alkaloids in coptidis rhizoma,then hydriding alkaloids with sodium borohydride, secondly, hy- droxylating alkaloids with Lewis acid,tetrahydroberberine can be obtained. The tetrahydroberberine can convert to tetrahydropal- matine by using methylbenzene as solvent, adding a small amount of several batches methyl iodide. Access to the tetrahydropalma- tine in overall yield is 86.3%. The results show that the synthesis of tetrahydroberberine is a workable solution.