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异三尖杉酯碱系三尖杉属植物中所含具有抗肿瘤活性的四种生物碱之一,其本身的合成已有三种不同的方法先后获得成功。但是,在这些合成中,生成的异三尖杉酯碱都是立体异构体的混合物。据报导异三尖杉酯碱及其某些类似物对癌细胞具有明显的抑制作用。为了考察这类化合物的结构与抗癌活性之间的关系,并为异三尖杉酯碱立体异构体构型的确定提供依据,我们进行了(2R,3R)-酒石酸甲酯三尖杉碱酯Ⅵ和(2S,3S)-酒石酸甲酯三尖杉碱酯Ⅶ的合成。合成路线如下:
Homoharringtonine base is one of the four alkaloids with anti-tumor activity contained in Cephalotaxus. Three different methods have been developed for their success. However, in these syntheses, alloharringtonine formed is a mixture of stereoisomers. It has been reported that homoharringtonine and some of its analogs have a significant inhibitory effect on cancer cells. In order to investigate the relationship between the structure of these compounds and anticancer activity, and to provide the basis for the determination of the isomer structure of homoharringtonine, we carried out (2R, 3R) - methyl tartrate Synthesis of Alkali Esters VI and (2S, 3S) - Methyl Tartrate. The synthetic route is as follows: