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process to produce macrolides with sostiutuenti ossidrilici capable of being acilati (076) isolated from the fermentation broth of a strain of streptomyces avermitilis.useful in particular as pesticides and the product obtained
process to produce macrolides with sostiutuenti ossidrilici capable of being acilati (076) isolated from the fermentation broth of a strain of streptomyces avermitilis.useful in particular as pesticides and the product obtained
The invention provides compounds having the formula CHEM 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.
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机译:本发明提供了具有化学式的化合物,其中虚线表示单键或双键; R1是羟基或酰氧基,并且仅当虚线表示单键时才存在; R 2为异丙基或仲丁基; R3是氢,甲基或酰基;并且R为氢,酰基,α-L-油烯基,4min-酰基-α-L-油烯基,4min-(α-L-油烯基)-α-L-油烯基,4sec-酰基-4min-( α-L-油烯基)-@-L-油烯基;上述定义受某些条件的限制。这些化合物是C-076的衍生物,其中取代基是某些芳族或非芳族酰基和C-076的单糖和糖苷配基。根据所取代的特定C-076化合物,通过各种方法制备酰基衍生物。单糖和糖苷配基化合物是通过酸水解母体C-076制备的。如此产生的化合物被用于其深远的驱虫,杀虫,除螨和杀螨活性,并公开了用于此类用途的组合物。
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