Anticancer 4':de-oxo 4':halo doxorubicin 14:ester(s) - prepd. by treating de-oxo halo:doxorubicin with bromine and an acid salt

摘要

4'-Deoxy-4'-halo doxorubicin 14-esters of formula (I) are new. R = acyl group derived from one of the following acids: mono- or di-carboxylic aliphatic, aromatic, cycloaliphatic, araliphatic, or heterocyclic, which may contain up to 20C atoms and may be substituted by any of the following: halogen, OH, alkyl, alkoxy, amino, mono or di alkylamino, nitro, alkyl or aryl carbonic acid, carbamic acid, alkyl carbamic acid, or sulphonic acid. - Prepn. has a 4'-deoxy-4'-halo daunorubicin dissolved in an anhydrous solvent and treated with bromine at ambient temp., to give the corresp. 14-bromo deriv. This is then treated with a salt ROM, where M is an alkali metal alkaline earth metal, quaternary ammonium, or quaternary alkyl ammonium, in an inert solvent.