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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Main Authors | , , , |
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Format | Patent |
Language | English |
Published |
11.02.1975
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Subjects | |
Online Access | Get full text |
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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. |
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Bibliography: | Application Number: CA19720132333 |