C-23-MODIFIED DERIVATIVES OF DMT

摘要

of the Invention C-23-Modified derivatives of demycinosyltylosin (DMT) or the formula: < IMG > wherein R is iodo, bromo, chloro, fluoro, -S-R4, azido, -NHR5, pyridinium or -OSO2CF3; R1 is hydrogen, optionally substituted C1-C5- alkanoyl or optionally substituted benzoyl, phenylacetyl, phenylpropiotlyl, phenoxyacetyl or phenylthioacetyl, R2 is hydrogen, optionally substituted C1-C5- alkanoyl or optionally substituted benzoyl, phenylacetyl or phenylproplonyl; R3 is hydrogen, optionally substituted C1-C5- alkanoyl or optionally substituted benzoyl, phenylacetyl or phenoxyacetyl; R4 is hydrogen, optionally substituted C1-C6- alkyl, cyclohexyl, C1-C5-alkanoyl, optionally substituted phenyl. or benzyl, or an optionally substituted heteroaryl group selected from imidazolyl, pyrazolyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, triazinyl, triazolyl, tetrazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, isothiazolyl, thiadiazolyl, thienyl and furanyl; and R5 is hydrogen or an acyl group selected from optionally substituted C1-C5-alkanoyl or optionally substituted benzoyl, phenylacetyl or phenylpropionyl; and salts thereof are useful antibiotics or intermediates to antibiotics.