| 摘要 |
<p>1348055 4,5 - Epoxy - bufadienolide glycosides FARBWERKE HOECHST AG 26 April 1971 [2 May 1970] 11374/71 Heading C2U The invention comprises compounds of formula (wherein R 1 is CH 3 , CHO, CH 2 OH, CH 2 O alkyl or CH 2 O acyl and R 2 is a mono-, di- or trisaccharide radical which may optionally be esterified, etherified, acetalized or ketalized); and their preparation (a) from the corresponding 4- hydroxy - 5 - halo compounds (wherein the 3-sugar radical is esterified) by dehydrohalogenaation, or (b) from the corresponding 3#-hydroxy compounds by reaction with an acylated 1- halo - 1 - deoxyglycose in the presence of a silver salt. Subsequently the sugar radical may be saponified, and the resulting free glycoside reacylated, etherified, acetalized or ketalized. 2<SP>1</SP>,3<SP>1</SP>,4<SP>1</SP> - Triacylates of 3# - (α- L - rhamnopyranosyloxy) - 4#,14 - dihydroxy - 5 - bromo- 5α,14# - bufa - 20,22 - dienolide are prepared from proscillaridin via proscillaridin 2<SP>1</SP>,3<SP>1</SP>,4<SP>1</SP>- triacylates. Specified acyl groups are formyl, acetyl, propionyl, butyryl, benzoyl and pnitrobenzoyl. 3#,14 - Dihydroxy - 4#,5 - epoxy - 5#,14#- bufa - 20,22 - dienolide is prepared from scillarenin by reaction with m-chloroperbenzoic acid. Compounds I are said to be cardioactive, and may be made up with carriers into pharmaceutical compositions for oral administration.</p> |
