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由3′-O-5-甲基-2-氧已酰基]-三尖杉碱(简称α-酮酰基三尖杉碱)(2)与溴代乙酸甲酯进行Reformatsky反应,顺利地得到脱氧三尖杉酯碱(1a)及表-脱氧三尖杉酯碱(1b)混合物,产率为60—70％,二者通过苦味酸盐分级结晶后,再分别转化成游离碱(1a)以及(1b)纯品,此外,还得到了外消旋α-酮酰基三尖杉碱(±2),由其制得外消旋脱氧三尖杉酯碱(±la)和外消旋表-脱氧三尖杉酯碱(±1b)的结晶纯品;它们的核磁共振谱、质谱、红外光谱(涂膜法)与对应的旋光异构体一致,红外光谱KBr压片法表明,(±1a)和(±1b)之间有明显的差异,为了获得关键中间体(2),探索了两条合成路线,均得到预期结果。
Reformatsky reaction of 3’-O-5-methyl-2-oxoacyl] -cisplatin (abbreviated as α-ketoacylcistrostat) with methyl bromoacetate gave deoxy The mixture of harringtonine (1a) and epi-dextrin harringtonine (1b) in a yield of 60-70%, both fractionated by picrates and then converted to the free base (1a) and (1b) pure, in addition, racemic α-ketoacylcephalitis (± 2) was also obtained, from which racemic deoxyharringtonine (± la) and racemic- (± 1b). Their NMR, MS and IR spectra (corresponding to the corresponding optical isomers) were consistent with the corresponding optical isomers. The results of IR spectrum KBr showed that (± 1a ) And (± 1b). In order to obtain the key intermediate (2), two synthetic routes were explored, both of which yielded the expected results.