李振肃, 王海青, 朱琪, 卓济苍. 5-孕甾烯-3β,17α-双醇-20-酮-3-醋酸酯-17α-脂肪酸酯类的合成及其构效关系研究J. 药学学报, 1983, 18(2): 119-124.
引用本文: 李振肃, 王海青, 朱琪, 卓济苍. 5-孕甾烯-3β,17α-双醇-20-酮-3-醋酸酯-17α-脂肪酸酯类的合成及其构效关系研究J. 药学学报, 1983, 18(2): 119-124.
LI Zhen-su, WANG Hai-qing, ZHU Qi , ZHUO Ji-cang, . SYNTHESIS OF 5-PREGNEN-3β, 17α-DIOL-20-ONE-3-ACET ATE-17α-CARBOX YLIC ACID ESTERS, AND STUDIES ON THEIR STRUCTURE-ACTIVITY RELATIONSHIPSJ. Acta Pharmaceutica Sinica, 1983, 18(2): 119-124.
Citation: LI Zhen-su, WANG Hai-qing, ZHU Qi , ZHUO Ji-cang, . SYNTHESIS OF 5-PREGNEN-3β, 17α-DIOL-20-ONE-3-ACET ATE-17α-CARBOX YLIC ACID ESTERS, AND STUDIES ON THEIR STRUCTURE-ACTIVITY RELATIONSHIPSJ. Acta Pharmaceutica Sinica, 1983, 18(2): 119-124.

5-孕甾烯-3β,17α-双醇-20-酮-3-醋酸酯-17α-脂肪酸酯类的合成及其构效关系研究

SYNTHESIS OF 5-PREGNEN-3β, 17α-DIOL-20-ONE-3-ACET ATE-17α-CARBOX YLIC ACID ESTERS, AND STUDIES ON THEIR STRUCTURE-ACTIVITY RELATIONSHIPS

  • 摘要: 本文报告薯蓣皂甙元的降解物孕甾双烯醇酮醋酸酯通过环氧化、开环反应所得开环物Ⅰ经20%钯-碳催化氢解脱溴反应合成Ⅱ,进而合成Ⅲ,Ⅳ(未知物)和Ⅴ,并对这些化合物做了抗炎作用的试验,探寻其结构与抗炎活性的关系。本文还对Ⅱ与酸性活性氧化铝或碱作用后的产物结构进行了初步确证。

     

    Abstract: The syntheses of 17α-carboxylic acid esters of 5-pregnen-3β, 17α-diol-20-one-3 -acetate Ⅲ, Ⅳ (not reported previously) and Ⅴ are described. Animal tests (inflammatory granuloma pouch) gave the following results: the propanoic acid ester Ⅳ showed significant anti-inflammatory action, nearly equivalent to that of Antiflamisonum. The caproic acid ester Ⅴ has been found to Be somewhat more active than Antiflamisonum. D-Homo products obtained from the action of acidic aluminum oxide or alkali on 5-pregnen-3β, 17α-diol-20-one 3-acetate (Ⅱ) are studied.

     

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