Mono- and diepoxide derivatives of LL-F28249 compounds

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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549264, A61K 3566

Patent

active

048762725

ABSTRACT:
The present invention relates to novel mono- C(26,27) and diepoxide C(14,15;26,27) derivatives of LL-F28249.alpha., .beta., .epsilon., .zeta., .theta. and .iota. compounds. The LL-F28249 compounds (collectively) are isolates from the fermentation broth of Streptomyces cyaneogriseus subspecies noncyanogenus having deposit accession number NRRL-15773. The compounds of this present invention are derived by regioselective epoxidation of 5,23-0,0-bis-silylated LL-F28249 compounds at low temperature, followed by desilylation. These novel compounds have anthelmintic, insecticidal, ectoparasiticidal, nematicidal and acaricidal activity and also are useful intermediates for the preparation of further biologically active compounds. Compositions containing these described derivatives as active ingredients thereof are described.

REFERENCES:
patent: 4530921 (1985-07-01), Mrozik

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