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甲基化防己诺林碱制备粉防己碱研究

Preparation of Tetrandrine by Methylation of Fangchinoline
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摘要 粉防己碱是一种治疗心血管疾病的药物,只能从中药粉防己中提取.近年来粉防己的资源量锐减.防己诺林碱的含量仅次于粉防己碱,至今还没有成为一种药物,是粉防己碱生产时的副产品.为了有效利用这种副产品,本文研究了将防己诺林碱转化为防己碱的方法.在不同的溶剂系统和碱性条件下,以防己诺林碱为原料,采用两种甲基化试剂制备了粉防己碱.结果表明,溶剂、碱性和甲基化试剂等对收率都有很大的影响.其中最优的方法是,硫酸二甲酯为甲基化试剂,二氯甲烷/KOH溶液为溶剂,收率最高,副反应最少,为61.4%.此转化反应能够有效利用粉防己药材. Tetradrine is a medicine that is used for cardiovascular diseases and can only be made from the Chinese folk medicine, Stephania tetrandra S. Moore. The natural resource of S. tetrandra has reduced rapidly in recent years. Fangchinoline is an alkaloid whose content is only less than the main component, tetrandrine in S. tetrandra and it is not used as medicine until now. It is a byproduct in tetrandrine manufacture. In order to use this byproduct, the method to convert fangchinoline into tetrandrine was investigated. Fangchinoline as starting material was methylized with two kinds of methylation reagents in different solvents and alkaline solu- tion. The results showed that the yield varied between 0 - 61.4% with solvents, alkalines and methylation reagents. The best yield (61.4%) and least sidereaction could be obtained by using dimethyl sulfate as the methylation reagent and CH2Cl2/KOH solution as solvents. This conversion could make it possible and effective to utilize S. tetrandra. Fig 2, Tab 4, Ref 19
出处 《应用与环境生物学报》 CAS CSCD 北大核心 2008年第2期258-260,共3页 Chinese Journal of Applied and Environmental Biology
关键词 粉防己碱 防己诺林碱 甲基化 粉防己 tetrandrine fangchinoline methylation Stephania tetrandra
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