| 摘要 |
The invention provides derivatives of C-076, which is a series of macrolides, having certain hydrocarbon substituents. The hydrocarbon substituents in general are alkyl groups which may be straight or branched and may optionally be substituted with phenyl. The substituted C-076 compounds are prepared by various procedures depending upon the position of the reaction site, and the particular C-076 compound being substituted. The compounds thus produced are of formula:
<CHEM>
where the broken line indicates that a single or a double bond is present in the 22(23) position; R1 is hydroxy, loweralkanoyloxy or hydrocarbonoxy and is present only when the broken line indicates a single bond; R2 is iso-propyl or sec-butyl; R3 is hydrogen, methyl, loweralkanoyl or a hydrocarbon;
R is hydrogen, loweralkanoyl, a hydrocarbon,
<CHEM>
where R4 is hydrogen, loweralkanoyl or a hydrocarbon, and
R5 is hydrogen or methyl; and the said hydrocarbonoxy group of R1 is an alkoxy of from 1 to 10 carbon atoms or an alkoxy of from 1 to 10 carbon atoms or an alkoxy of from 1 to 10 carbon atoms substituted by phenyl and the said hydrocarbon groups of R and R4, which are the same or different, are alkyl of from 1 to 10 carbon atoms or alkyl of from 1 to 10 carbon atoms substituted by phenyl; and the said hydrocarbon group of R3 is an alkyl of from 2 to 10 carbon atoms or an alkyl of from 1 to 10 carbon atoms substituted by phenyl; provided that at least one of the R, R1, R3, and R4 groups is or contains a hydrocarbon group or R5 is methyl. They have profound anthelmintic, insecticidal, ectoparasiticidal and acaracidal activity and compositions for such uses are also disclosed. |
