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三尖杉酯碱对急性、慢性粒细胞和单核细胞性白血病有较好疗效。由三尖杉碱合成的三尖杉酯碱为一对差向异构体,即三尖杉酯碱(2′R)和表三尖杉酯碱(2′S)。为了考察并比较此二差向异构体单独使用与合并使用时的生理活性,需要制备出一定量单体纯品,同时要求建立一个简便快速的分析方法,以供选择良好的反应条件与分离条件和较准确地评价药物临床疗效。本文报告了半合成三尖杉酯碱两个差向异构体的分离制备方法与分析方法。即将半合成三尖杉酯碱制成盐酸盐用硅胶制备薄层,展开剂为二氯乙烷-甲醇(4:1)再加适量盐酸调节 pH 近4,分离得到酯碱(2′R)
The harringtonine has a good effect on acute and chronic granulocyte and monocytic leukemia. The harringtonine base synthesised from harringtonine is a pair of epimers, namely harringtonine (2’R) and epidaunase (2’S). In order to investigate and compare the physiological activities of the two epimers when used alone and in combination, it is necessary to prepare a certain amount of monomeric pure product, and at the same time, it is required to establish a simple and rapid analytical method for selecting a good reaction condition and separation. Conditions and more accurate evaluation of clinical efficacy of drugs. This paper reports the preparation and analysis methods for the separation of two epimers of semisynthetic harringtonine. A semi-synthetic harringtonine base was prepared into a thin layer of silica gel with a dichloroethane-methanol (4:1) solution and an appropriate amount of hydrochloric acid to adjust the pH to approximately 4 to separate the ester base (2′R). )