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目的:制备甘草次酸类衍生物30-三苯甲基-11-脱氧甘草萜醇(Ⅴ)。方法:对甘草次酸(Ⅰ)进行化学结构修饰,制备11-脱氧甘草萜醇(Ⅳ),并将它与三苯氯甲烷缩合而制备目标化合物——30-三苯甲基-11-脱氧甘草萜醇(Ⅴ)。结果:通过还原、脱水、催化氢化和缩合反应获得目标化合物(Ⅴ),经鉴定其(Ⅴ)为甘草萜醇类新化合物,反应产率达46%。结论:三苯氯甲烷在三乙胺和二甲氨基吡啶等碱性催化下与甘草萜醇的C30-位羟基进行选择性缩合反应,此反应产率较与C3-位羟基化反应的要高,此种反应条件在甘草萜醇C30-位羟基的选择性保护中具有重要的价值。此外,利用还原剂Red-Al对甘草次酸进行还原修饰要比用四氢锂铝容易、产率高。
OBJECTIVE: To prepare glycyrrhetic acid derivative 30-trityl-11-deoxy licoricetiol (Ⅴ). Methods: The glycyrrhetinic acid (Ⅰ) was chemically modified to prepare 11-deoxy lictrinterol (Ⅳ) and condensed with triphenylchloromethane to prepare the target compound -30-trityl-11- Glycyrrhizin alcohol (Ⅴ). Results: The target compound (V) was obtained by reduction, dehydration, catalytic hydrogenation and condensation reaction. It was identified that (Ⅴ) was a new glycyrrhizin alcohol compound with a yield of 46%. CONCLUSION: Triphenylmethyl chloride is selectively condensed with hydroxyl of C 30 -hydroxyl of licoricetiol under basic catalysis, such as triethylamine and dimethylaminopyridine. The yield of this reaction is higher than that of the hydroxylation of C3-position , Such reaction conditions in the glycyrrhizin alcohols C30-position hydroxyl selective protection has an important value. In addition, the use of reductant Red-Al glycyrrhetinic acid reduction than the use of lithium aluminum tetrahydrate easy, high yield.