| 摘要 |
A method of making compounds of the formulae: <IMAGE> wherein X is <IMAGE> R1 is hydrogen, methyl, C1-10 alkoxycarbonyl or arylsulfonyl when X is CH3CH2CHNH2 and is additionally aralkoxycarbonyl when X is NH2; one of R2 and R3 is hydrogen and the other is OH, NHR1 or NMeR1 where R1 is as defined above; R4 is hydrogen or C1-10 alkyl when X is CH3CH2CHNH2 and is additionally aralkyl when X is NH2; R5 is hydrogen or C1-3 alkyl when X is CH3CH2CHNH2; R5 is hydrogen when X is NH2; one of R6 and R7 is hydrogen and the other is methyl except when X is CH3CH2CHNH2 and R2 is H, in which case R6 is methyl and R7 is hydrogen. These compounds are made from erythromycin-derived fragments of the formulae: <IMAGE> +TR <IMAGE> where R1, R2, R3 and R4 are defined as before for when X is NH2; R5 is hydrogen or C1-3 alkyl; if R5 is hydrogen, then R6 is methyl and R7 is hydrogen and the two structures above exist in equilibrium with each other; if R5 is alkyl, then one of R6 and R7 is hydrogen and the other is methyl and the compound exists only as the structure on the above left.
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