PROCEDE POUR LA PREPARATION DES DERIVES DE 22-FLUOR-DIGOXINE

摘要

1363033 22-Fluorodigoxin derivatives DR KARL THOMAE GmbH 8 Sept 1972 [11 Sept 1971] 41889/72 Heading C2U The invention comprises compounds of formula wherein one of R 1 and R 2 is H and the other is C 1-3 alkyl; or R 1 is H and R 2 is C 1-5 aliphatic carboxylic acyl; or R 1 and R 2 together represent >C(A)(B) where A and B are each H or alkyl (at least one being alkyl), or A, B and the intervening carbon atom together represent a 5- or 6-membered alicyclic ring; or R 1 and R 2 together represent >C(OR 3 )(R 4 ) where R 3 is alkyl and R 4 is H or a C 1-4 alkyl group. Compounds (I) are prepared from 22-fluorodigoxin by alkylation, acetalization, ketalization, esterification or orthoesterification. Preferably, the 3111-monoesters are prepared via the 3111,4111-orthoesters. 22-Fluorodigoxin is prepared as described in Specification 1,320,361. Compounds (I), with the exception of those wherein R 1 and R 2 represent >C(OR 3 )(R 4 ), are said to be cardioactive, and may be made up with carriers into pharmaceutical compositions fororal, rectal and parenteral administration. Reference has been directed by the Comptroller to Specification 1,320,361.