发明名称 Delta<4,20,22>-BUFATRIENOLIDE-RHAMNOSIDE-ACYLATES AND PROCESS FOR THEIR PREPARATION
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 3<SP>1</SP>-monoacylate. The temporary ketalization of the 2<SP>1</SP>,3<SP>1</SP>-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.
申请公布号 GB1286232(A) 申请公布日期 1972.08.23
申请号 GB19700000770 申请日期 1970.01.07
申请人 KNOLL A.G. CHEMISCHE FABRIKEN 发明人
分类号 A61K31/58;A61K31/585;A61K31/70;A61K31/704;A61P9/04;B60R25/02;C07J19/00 主分类号 A61K31/58
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