ACYL DERIVATIVES OF THE DIGOXIN AND PROCESS FOR THE PRODUCTION THEREOF

1371937 Digoxin 3111-esters BOEHRINGER INGELHEIM GmbH 13 Jan 1972 [14 Jan 1971] 1729/72 Heading C2U The invention comprises digoxin 3111-eaters of formula wherein R 1 is the remainder of the digoxin molecule; and R 2 is C 1-4 alkyl substituted by halo, aryl or cycloalkyl, or R 2 is C 2-12 alkyl or C...

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Bibliographic Details
Main Authors LOESEL, WALTER, HOEFKE, WOLFGANG, TRAUNECKER, WERNER, MERZ, HERBERT
Format Patent
LanguageEnglish
Published 11.02.1975
Subjects
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
STEROIDS
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Summary:1371937 Digoxin 3111-esters BOEHRINGER INGELHEIM GmbH 13 Jan 1972 [14 Jan 1971] 1729/72 Heading C2U The invention comprises digoxin 3111-eaters of formula wherein R 1 is the remainder of the digoxin molecule; and R 2 is C 1-4 alkyl substituted by halo, aryl or cycloalkyl, or R 2 is C 2-12 alkyl or C 3-8 cycloalkyl. Compounds I are prepared from digoxin either (i) by conventional direct acylation to give a mixture of 3111- and 4111-esters which is resolved by column chromatography, Craig distribution and/or crystallisation whereafter the 4111-isomer maybe isomerized to the 3111-isomer with activated aluminium oxide in an inert solvent; or (ii) by reaction with a trialkyl orthoester and selective hydrolysis of the resulting compound of formula wherein R 3 is C 1-6 alkyl. Cardioactive compositions for oral, rectal and parenteral administration comprise a compound of Formula I and a carrier.
Bibliography:Application Number: CA19720132333