ANALOGIFREMGANGSMAADE TIL FREMSTILLING AF MONOACYL-DERIVATER AF C-076 MAKROLIDER

The invention provides compounds having the formula in which the broken line indicates a single or a double bond; R1 is hydroxy or acyloxy and is present only when the broken line indicates a single bond; R2 is iso-propyl or sec-butyl; R3 is hydrogen, methyl or acyl; and R is hydrogen, acyl, alpha -...

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Bibliographische Detailangaben
Hauptverfasser: GEORGE ALBERS-SCHONBERG, HELMUT HUGO MROZIK, PETER KULSA, MICHAEL HERBERT FISHER
Format: Patent
Sprache:dan
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Zusammenfassung:The invention provides compounds having the formula in which the broken line indicates a single or a double bond; R1 is hydroxy or acyloxy and is present only when the broken line indicates a single bond; R2 is iso-propyl or sec-butyl; R3 is hydrogen, methyl or acyl; and R is hydrogen, acyl, alpha -L-oleandrosyl, 4 min -acyl- alpha -L-oleandrosyl, 4 min -( alpha -L-oleandrosyl)- alpha -L-oleandroxyl, 4 sec -acyl-4 min -( alpha -L-oleandrosyl)- @-L-oleandroxyl; the above definitions being subject to certain provisos. These compounds are derivatives of C-076 in which the substituents are certain aromatic or non-aromatic acyl groups and the monosaccharide and aglycone of C-076. The acyl derivatives are prepared by various procedures depending upon the particular C-076 compound being substituted. The mono-saccharide and aglycone compounds are prepared by acid hydrolysis of the parent C-076. The compounds thus produced are used for their profound anthelmintic, insecticidal, ectoparasiticidal and acaracidal activity and compositions for such uses are also disclosed.