process for the preparation of pharmaceutical preparations which contain bufatrienoliderhamnoside ethers, and method for the preparation of these bufatrienoliderhamnoside ethers.

摘要

1,266,251. Butatrienolide rhamnoside ethers. KNOLL A.G. CHEMISCHE FABRIKEN. 25 Feb., 1970 [28 Feb., 1969], No. 8979/70. Heading C2U. The invention comprises compounds of formula wherein R is Me or formyl; R 1 and R 2 are each H, acetyl or C 1-6 alkyl or together form isopro pylidene; and R 3 is H, acetyl or C 1-6 alkyl; provided that at least one of R 1 , R 2 and R 3 is C 1-6 alkyl. Preparation of the above is by reaction of a C 1-6 alkyl halide with proscillaridin, 19-oxoproscillaridin or the acetonide of either, followed when required by acetylation. When mixtures of products are obtained, these may be separated by recrystallization, column chromatography and/or Craig distribution. Monoethers obtained may be subjected to further etherification. 2SP1/SP,3SP1/SP-o-Isopropylidene-4-o-alkyl products may be acidified to cleave the isopropylidene group. Reference is made to the cleavage of certain products with NalO 4 . The inventive compounds are stated to be cardioactive and may be made up with carriers into pharmaceutical compositions for oral administration.