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US 4,201,861 AGranted
Acyl derivatives of C-076 compounds
AssigneeMerck & Co., Inc.
InventorsHelmut H. Mrozik, Michael H. Fisher, Peter Kulsa
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Abstract
Derivatives of C-076, a series of macrolides, are described in which the substituents are acyl groups. The acyl substituents may be aromatic of non-aromatic. The acyl derivatives are prepared by various procedures depending upon the particular C-076 compound being substituted. The compounds thus produced have profound anthelmintic, insecticidal, ectoparasiticidal and acaracidal activity and compositions for such uses are also disclosed.
Claims16
A compound having the formula:
- ##STR5## wherein the broken line indicates a single or a double bond;
- R.sub.1 is hydroxy or acyloxy and is present only when the broken line indicates a single bond;
- R.sub.2 is iso-propyl or sec-butyl;
- R.sub.3 is hydrogen, methyl or acyl;
- and
- R is hydrogen, acyl, .alpha.-L-oleandrosyl, 4'-acyl-.alpha.-L-oleandrosyl, 4'-(.alpha.-L-oleandrosyl)-.alpha.-L-oleandrosyl, 4"-acyl-4'-(.alpha.-L-oleandrosyl)-.alpha.-L-oleandrosyl;
- provided that at least one of the R, R.sub.1 or R.sub.3 groups contains an acyl group, and further that said acyl and the acyl portion of said acyloxy group is selected from loweralkanoyl;
- substituted loweralkanoyl wherein the substituents are halogen, carboxy, loweralkoxycarbonyl, amino, mono- or di-loweralkylamino, or loweralkanoylamino;
- unsaturated loweralkanoyl, loweralkoxycarbonyl, halogenated loweralkoxycarbonyl, benzoyl, or substituted benzoyl in which the substituents are halogen, nitro, alkyl, amino, hydroxy or alkoxy;
- carbamoyl, and N-substituted and N,N-disubstituted carbamoyl wherein the substitution is loweralkyl, benzyl, hydroxyloweralkyl or the carbamoyl nitrogen may be incorporated into a morpholine heterocycle.
7 more elements
Dependencies are inferred from the claim text.