C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/312
C07D 257/06 (2006.01)
Patent
CA 1161044
ABSTRACT OF THE DISCLOSURE: The present invention relates to a process for the preparation of a compound of the formula (I) Image (I) where the squiggly bond between carbon atoms 14 and 15 is an all-E-link or 13-Z-link, and of its physiologically tolerated salts, wherein a reactive retinoic acid deriv- ative of the formula (II) Image (II) where the squiggly bond between carbon atoms 14 and 15 is an all-E-link or 13-Z-link and R is a halogen or an N- oxysuccinimide group, is reacted with 5-aminotetrazole, advantageously in a solvent and in the presence or absence of an acid acceptor, and, if desired, the resulting compound is converted to a physiologically tolerated salt by means of a base, or wherein all-E-retinoic acid or 13-Z-retinoic acid of the formula (III) Image (III) is condensed with 5-aminotetrazole in a solvent in the presence of a suitable dehydrating agent which activates the carboxyl yroup and which is of the type used in peptide synthesis, and, if desired, the resulting compound is converted to a physiologically tolerated salt by means of a base, and pharmaceutical formulations which contain compounds of formula I and salts and which may, in particular, be used in the treatment of neoplasias, acne, dermatoses, psoriasis, dermatological disorders and rheumatic conditions.
368875
Frickel Fritz-Frieder
Nuerrenbach Axel
Basf Aktiengesellschaft
Robic Robic & Associes/associates
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