NOVEL METHOD OF PRODUCING 7-(SUBSTITUTED)-9[(SUBSTITUTED GLYCYL)- -AMIDO]-6-DEMETHYL-6-DEOXYTETRA-CYCLINES

摘要

The invention provides a novel method for producing 7-(substituted)-9-[(substituted glycyl)amido]-6-demethyl-6- deoxytetracyclines (formula I). 9-amino-7-(subst.)-6- demethyl-6-deoxytetracyclines (formula III) reacts with halogen-acyl-halogenide Y(CH2)nC(O)Q, where Q is halogen and Y is halogen-alkyl with C1-4, on the proviso that n = 0, and halogen or O-toluene, O-methyl- or tri-fluorine-methyl-sulphonate, on the proviso that n = 1-4, and accrued 9-[(halogen-acyl)amido]-7- (subst.)-6-demethyl-6-deotetracycline (II) reacts with nucleofile R4H.