Mono and diacyl derivatives of LL-F28249 Compounds

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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C07D31500

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active

051498324

ABSTRACT:
The present invention relates to novel 5-acyl, 23-acyl and 5,23-diacyl derivtaives of the LL-F28249 compounds. These LL-F28249 compounds (collectively) are isolates from the fermentation broth of Streptomyces cyaneogriseus subspecies noncyanogenus having deposit accession number NRRL 15773. The present 5-acyl and 5,23-diacyl compounds are prepared by selective acylation using acid chlorides or anhydrides in the presence of 4-dimethylaminopyridine. The 23-acyl compounds are prepared by selective acylation of the 5-O-silylated LL-F28249 compounds. These novel compounds have potent anthelmintic, insecticidal, ectoparasiticidal, nematicidal and acaricidal activity. Compositions containing these derivatives of LL-F28249 also are described herein.

REFERENCES:
patent: Re32034 (1985-11-01), Chabala et al.
patent: 4201861 (1980-05-01), Mrozik et al.
H. Mrozik et al, J. Med. Chem. (1982), vol. 25, pp. 658-662.

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