5-azolylacetoxymilbemycins as ecto- and endoparasites

Details 5-azolylacetoxymilbemycins as ecto- and endoparasites 5-azolylacetoxymilbemycins as ecto- and endoparasites

1985-11-18

1987-09-29

Hollrah, Glennon H.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514382, 514383, 514359, 514397, 514407, 548262, 548253, 548255, 548336, 548374, 548101, 549264, C07D24908

Patent

active

046969225

ABSTRACT:
The present invention relates to milbemycin derivatives of the formula I ##STR1## wherein X is hydrogen or .beta.-halogen, R is methyl, ethyl, isopropyl or sec-butyl and Az is a 5 membered heterocyclic aromatic ring which contains 2-4 nitrogen atoms and is attached in the 1-position and which is unsubstituted or substituted by one or two C.sub.1 -C.sub.6 alkyl groups. These compounds, and the acid addition salts and metal complexes thereof, are effective pesticides for controlling endo-and ectoparasites, especially for controlling neamatodes which are parasites of animals. The may be obtained by appropriate esterification in 5-position of milbemycin derivatives. The selective .beta.-halogenation of 14,15-epoxymilbemycin derivatives can be effected via the intermediate .DELTA..sup.13,14 -15-hydroxymilbemycins with appropriate halogenating agents.

REFERENCES:
Tetrahedron Letters, 24, p. 5333, by H. Mrozik, (1983).

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