process for the production of new 3 - amino - 4 - dehydro cardenoliden

摘要

1363674 3-Aminocardenolides FARBWERKE HOECHST AG 27 Oct 1971 [29 Oct 1970] 49965/71 Heading C2U The invention comprises compounds of formula wherein R 1 is H or C 1-4 aliphatic carboxylic acyl; R 2 and R 3 are each H or OH, or R 2 and R 3 together represent an - or #-epoxy group or #SP14/SP-unsaturation; R 4 , R 5 and R 7 are each H or free or esterified hydroxyl; R 6 is H or free, esterified or etherified hydroxyl; and R 8 is H or OH; and salts of those compounds wherein R 1 is H. Compounds I are prepared from the corresponding 3-ones (which may also contain a 19- oxo group) by reaction with hydroxylamine or a salt thereof to give a 3-oxime which is reduced using zinc in the presence of an aliphatic carboxylic acid to give a 3-amino and/or 3-acylamino compound I. The 3-acylamino compounds (and mixtures thereof with the 3-amino compounds) may be hydrolysed to give the 3- amino compounds and the latter may be salified or acylated. The inventive compounds are said to be cardiotonic, and may be made up with carriers into pharmaceutical compositions for oral and parenteral administration.