| 摘要 |
The invention comprises canarigenin 3-monoglycosides having a 2-desoxy-sugar as the sugar component, and a process for preparing cardioactive cordenolide 3-monoglycosides having a 2-desoxy-sugar as the sugar component by enzymatic degradation of the diglycosides extracted from Digitalis canariensis L. to a mixture of the corresponding 3-monoglycosides and, if desired, separating the monoglycoside mixture into its components. Enzymes specified are strophanthobiase, digilanidase, digipurpidase, scillarenase, takadiastase and glucosidases. By chromatographic separation of the monoside mixture there are obtained canarigenin - 3 - digitoxoside, canarigenin - 3 - canaroside, and xysmalogen-3-canaroside. Canarigenin, canarigenin-3-methyl ether and 3-epicanarigenin are obtained as by-products from the above chromatographic separation. Canarigenin, 3-epicanarigenin and 3,5-dianhydroperiplogenin are obtained by treating canarigenin-3-digitoxoside with acetone-water and glacial acetic acid. Canarigenin-3-methyl ether is obtained by treating canarigenin-3-digitoxoside with methanol-water and glacial acetic acid. 3,5-Dianhydroperiplogenin is obtained by treating canarigenin-3-digitoxoside with methanol and dilute sulphuric acid on a steam bath. 31,41 - Di - (O - acetyl - ) - canarigenin - 3 - digitoxoside is obtained by acetylating canarigenin-3-digitoxoside by acetic anhydride in pyridine. Anhydroperiplogenone is prepared by cantions dehydrogenation of canarigenin. 3-Acetyl canarigenin is also prepared. Diglycoside starting material extraction from Digitalis canariensis L. is described. Canargenin-3-digitoxoside has cardioactive activity and may be used in combination with a pharmaceutical carrier in forms suitable for oral, parenteral or rectal administration, e.g. as tablets, capsules, dragees, ampoules, solutions, suspensions, emulsions or suppositories.
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