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2-氧代-6-甲基庚酰基三尖杉碱(3)与O-(1-甲氧基异丙基)羟基乙酸甲酯(4)在强碱性试剂二异丙胺锂(LDA)存在下,起亲核加成反应,反应中间体5在室温用酸性丙酮水解,得到一种新的三尖杉酯类生物碱——高异三尖杉酯碱(6c)及其立体异构体(6a、6b、6d)的混合物,产率56％、通过制备薄层层析分得这四个立体异构体,它们的~1H NMR和异三尖杉酯碱及其立体异构体的~1H NMR类似,推定了它们的绝对构型.初步药理试验表明,高异三尖杉酯碱及其立体异构体的混合物对白血病L7712的DNA合成有明显的抑制作用.
Methyl heptanoic acid (3) and O- (1-methoxyisopropyl) glycolic acid methyl ester (4) were reacted in the presence of strong base reagent lithium diisopropylamide (LDA) In the presence of a nucleophilic addition reaction, the intermediate 5 is hydrolyzed with acidic acetone at room temperature to obtain a novel homoharringtonine-homoharringtonine (6c) and its stereoisomerism The mixture of compounds (6a, 6b, 6d) was obtained in 56% yield and the four stereoisomers were separated by preparative thin layer chromatography, their 1H NMR and homoharringtonine bases and their stereoisomers ~ 1H NMR similar to presumed their absolute configuration.Primary pharmacological experiments show that homo homoharringtonine and its stereoisomers mixture of leukemia L7712 DNA synthesis was significantly inhibited.