Felippone F, Resnati G, Scolastico C, Tronconi G
Steroids. 1984 Mar;43(3):271-82. doi: 10.1016/0039-128x(84)90045-x.
A series of 2-carboxy-1, 4-androstadien-3-one derivatives and their alkyl esters, were prepared by high-yield syntheses. The compounds were structurally identified by physical methods. All these steroids are characterized by a marked antiglucocorticoid activity that proved long-acting in the case of the ester derivatives. 2-Carboxy-11 beta, 17 beta-dihydroxy-17-methyl-1, 4-androstadien-3-one or roxibolone, and its n-decylester or decylroxibolone, are the most promising derivatives in consideration of their pharmacological properties.
通过高产率合成方法制备了一系列2-羧基-1,4-雄甾二烯-3-酮衍生物及其烷基酯。通过物理方法对这些化合物进行了结构鉴定。所有这些甾体的特征在于具有显著的抗糖皮质激素活性，事实证明酯衍生物具有长效作用。考虑到其药理特性，2-羧基-11β,17β-二羟基-17-甲基-1,4-雄甾二烯-3-酮或罗昔勃龙及其正癸酯或癸基罗昔勃龙是最有前景的衍生物。
