Milbemycin ether derivatives, their preparation and their therapeutic and agrochemical uses.

摘要

Compounds of formula (I): <CHEM> in which: R<1> is a variety of organic groups; R<2> is hydrogen, halogen, cyano, nitro, optionally substituted alkyl, alkoxy, alkoxyalkoxy, or a group of formula: (CH2)nNHR<9> (CH2)nNR<9>COR<6> (CH2)nNR<9>COCOR<6> (CH2)nNR<9>COCOOR<7> (CH2)nNR<9>CHR<6>NHCOR<6> (CH2)nNR<9>CHR<6>NHCONHR<6> (CH2)nNR<9>CHR<6>NHCOOR<7> (CH2)nNR<9>C(=Y)YR<6> (CH2)nNR<9>C(=Y)NR<6>R<6> (CH2)nNR<9>C(=Y)NR<6>NR<6>R<6> (CH2)nNR<9>C(=Y)NR<6>NHZ (CH2)nNR<9>C(=NR<1><0>)NHR<1><0> (CH2)nNR<9>C(=NR<1><0>)R<6> or (CH2)nNR<9>SOmR<6> (in which m is 1 or 2; n is 0, 1 or 2; R<6> is a variety of organic groups; R<7> is alkyl, cycloalkyl, or aralkyl; R<9> is hydrogen or alkyl; R<1><0> is any of R<6>, or cyano, nitro, -COOR<7>, or -COR<6>; Y is oxygen or sulphur; Z is -COOR<7>, -COR<6> or -SO2R<6>); Q is methylene, ethylene or -OCH2-; P is methylene, ethylene, oxygen or a single bond; V and W each represents methylene, carbonyl or thiocarbonyl; R<3> and R<4> are hydrogen, alkyl or alkoxy; R<1><1> is alkyl, alkoxy, alkylthio, alkanoyloxy, alkoxycarbonyl, halogen, cyano, nitro, amino, mono- or di- alkylamino, carbamoyl, mono- or di- alkylcarbamoyl, or alkanoylamino; R<1><2> is hydrogen or alkyl; R<1><3> is alkyl; R<5> is methyl, ethyl, isopropyl or sec-butyl; and X is hydroxy, alkanoyloxy or hydroxyimino] and salts and esters thereof have valuable anthelmintic, acaricidal and insecticidal activities. Methods of preparing the compounds are also provided.