A PROCESS FOR PREPARING ANTRACYCLINE GLYCOSIDES

摘要

A process for prepg. antracycline glycosides of formula (I) comprises condensn. of 4-methoxy-daunomycinone with 2,3,6-trideoxy3- trifluoroacethylamino-4-O-methyl-L-lyxo-(or -L-arabino)- hexopyranosyl chloride in the presence of F3C-SO3Ag and a molecular sieve, in anhydrous CH2Cl2; followed by cleavage of the protective gp. with aq. NaOH; and opt. bromination of the side chain, followed by reaction of the protective gp. with aq. NaOH; and opt. bromination of the side chain, followed by reaction of the 14-bromo deriv. with NCOONa to give the 14-hydroxy cpd.. (I) and their acid addn. salts are useful as antitumor agents.