METHOD OF PREPARING ADENOSINE DERIVATIVES

摘要

1313459 Adenosine derivatives BOEHRINGER MANNHEIM GmbH 2 Dec 1971 [8 Dec 1970] 56025/71 Heading C2C Novel compounds of formula I wherein R 1 is a hydrogen or halogen atom, R 2 is a hydrogen or halogen atom or a hydroxyl group or an alkyl or alkoxy radical, R 3 is a a hydrogen atom or the group -CO-R 4 , wherein R 4 is an aryl radical which is optionally substituted one or more times by halogen atoms and/or alkyl, alkoxy and/or hydroxyalkyleneoxy radicals, A is a straight-chained or branched alkylene radical containing up to 3 carbon atoms and X is a valency bond or an oxygen atom; and the physiologically compatible salts thereof are prepared by one of the following methods:-(a) a compound of Formula III is reacted with a compound of Formula II wherein Z is halogen or a reactive mercapto group, or protected derivative thereof; (b) a compound of formula H 2 N-NHR 3 is reacted with a compound of formula wherein R 5 is alkyl, or a protected derivative thereof; or (c) a compound of Formula IV which may be prepared in situ by reaction of an optionally protected adenosine and a compound of Formula VII wherein Y is e.g. halogen, is heated in alkaline solution, e.g. aqueous ammonia, and in all cases protecting groups are saponified if necessary, and salts may be prepared in known manner. Intermediates of Formula VII above are prepared by reaction of a benzoic acid hydrazide NH 2 NHR 2 and a haloalkylbenzoyl bromide. Pharmaceutical compositions in conventional forms for enteral or parenteral administration, having a good effect on blood circulation and ability to lower the level of serum lipids, comprise an above novel compound and a diluent or carrier.