Valcavi U, Corsi B, Caponi R, Innocenti S, Martelli P
J Med Chem. 1975 Dec;18(12):1258-61. doi: 10.1021/jm00246a020.
In order to determine the influence of a 6alpha-methyl group activity, the 6alpha-methyl derivative of digitoxigenin 3-acetate 14 was prepared and pharmacologically tested in comparison with digitoxigenen 3-acetate. The synthesis of 6alpha-methyldigitoxigenin 3-acetate (14) was performed starting from 21-hydroxy-4-pregnene-3,20-dione (1). According to the cardiac activity determined on guinea-pig isolated heart and by slow infusion in the cat, the 6alpha-methyldigitoxigenin 3-acetate (14) is not more active than digitoxigenin 3-acetate.
为了确定6α-甲基基团活性的影响，制备了洋地黄毒苷元3-乙酸酯14的6α-甲基衍生物，并与洋地黄毒苷元3-乙酸酯进行了药理测试。6α-甲基洋地黄毒苷元3-乙酸酯（14）的合成从21-羟基-4-孕烯-3,20-二酮（1）开始。根据在豚鼠离体心脏上测定的心脏活性以及在猫身上缓慢输注的结果，6α-甲基洋地黄毒苷元3-乙酸酯（14）的活性并不比洋地黄毒苷元3-乙酸酯更强。
