Prisbe E J, Verheyden J P, Montgomery W W, Strosberg A M
J Med Chem. 1986 Feb;29(2):239-44. doi: 10.1021/jm00152a012.
The syntheses of the title compounds were accomplished by Koenig-Knorr condensation of acylated furanoses with digitoxigenin followed by basic hydrolysis of protecting groups. In this manner the riboside, 5-amino-5-deoxyriboside, 3,6-anhydroglucoside, and 3,6-dideoxy-3,6-iminoglucoside of digitoxigenin were prepared. These compounds as well as several of the synthetic intermediates showed weak to moderate cardiotonic activity.
通过酰化呋喃糖与洋地黄毒苷元的柯尼希-克诺尔缩合反应,随后对保护基团进行碱性水解,完成了标题化合物的合成。通过这种方式制备了洋地黄毒苷元的核糖苷、5-氨基-5-脱氧核糖苷、3,6-脱水葡萄糖苷和3,6-二脱氧-3,6-亚氨基葡萄糖苷。这些化合物以及几种合成中间体表现出弱至中等强度的强心活性。