C-23-MODIFIED DERIVATIVES OF OMT

摘要

of the Invention C-23-Modified derivatives of 5-O-mycaminosyl-tylonolide (OMT) of the formula: < IMG > wherein R is -S-R4, -NHR5, pyridinium, or -OSO2CF3; R1 is hydrogen, optionally substituted C1-C5- alkanoyl or optionally substituted benzoyl, phenylacetyl, phenylpropionyl, phenoxyacetyl or phenylthioacetyl; R2 and R3 are hydrogen, optionally substituted C1-C5-alkanoyl or optionally substituted benzoyl, phenylacetyl or phenylpropionyl; R4 is hydrogen, optionally substituted C1-C6- alkyl, cyclohexyl, C1-C5 alkanoyl, optionally substituted phenyl or benzyl; and R5 is hydrogen or an acyl group selected from optionally substituted C1-C5-alkanoyl, optionally substituted benzoyl, phenylacetyl, or phenylpropionyl or optionally substituted phenylglycyl or phenylalanyl; and of the formula: < IMG > wherein: R6 and R7 together form a CH2= group or R6 is R8O- and R7 is methyl; R8 is C1-C4-alkyl, benzyl or phenethyl; and R1, R2 and R3 are as defined in formula 1; and salts thereof are useful antibiotics or intermediates.