Verfahren zur Herstellung von 4,20,22-Bufatrienolidrhamnosidacylaten

摘要

1286232 Cardiac glycosides KNOLL AG CHEMISCHE FABRIKEN 7 Jan 1970 [9 Jan 1969 31 May 1969] 770/70 Heading C2U The invention comprises compounds of formula (wherein either (i) R is CH 3 or CHO and one or two of R 1 , R 2 and R 3 is carboxylic acyl of at least two carbon atoms, the other(s) being hydrogen; or (ii) R is CHO and R 1 , R 2 and R 3 are all acetyl), and their preparation by acylation of proscillaridin or 19-oxoproscillaridin. When mixtures of products are obtained these are separated by column chromatography and/or Craig division. Triacylates of proscillaridin may also be formed by the reaction. The exact nature of the product is determined by the reaction conditions. The presence of a boron complexing agent (e.g. ortho- or metaboric acid) results in a 31-monoacylate. The temporary ketalization of the 21,31-diol grouping during acylation results in a 41-monoacylate. The inventive compounds are said to be cardioactive and may be made up into compositions for oral administration.