| abstract |
In the present invention there are disclosed in position 13- substituted milbemycin-5-oxime derivatives of the general formula I, in which Re1 represents methyl, ethyl, isopropyl or secondary butyl; X represents carbonyl or methylene; Z represents =C=(Re2)i2 or =C=(CHi2)im (wherein Re2 represents alkyl and m is an integer of 2 to 5); n is 0 or 1; Re3 represents nitro, amino, alkylamino, dialkylamino, alkoxy, alkoxyalkoxy or the group of the general formulae iii, iv, v, vi, vii, viii or ix (wherein Re4 represents alkyl, substituted alkyl, cycloalkyl containing 3 to 6 carbon atoms, substituted cycloalkyl, alkenyl, alkynyl, carbocyclic aryl or a heterocycle; Re5 represents hydrogen or alkyl; Re6 represents hydrogen, alkyl or cycloalkyl; Re7 represents alkyl, cycloalkyl, a carbocyclic aryl or aralkyl; or Re6 and Re7 form together with a nitrogen atom to which they are attached a heterocycle; Y represents oxygen or sulfur; r is 1, 2 or 3; Q represents methylene or carbonyl; Re8 represents alkyl or a carbocyclic aryl; Re9 represents alkyl, cycloalkyl, a carbocyclic aryl or aralkyl; Re10 represents a heterocycle; and Re11 represents alkyl). The invented derivatives exhibit significant acaricidal, insecticidal and antihistaminic activity. |