PROCESS FOR PRODUCTION OF DERIVATIVES OF 13,3-MILBEMYCIN AND MEDICAL PREPARATIVES CONTAINING THEREOF

摘要

The invention relates to parasiticidally and insecticidally highly active compounds of formula I IMAGE (I) wherein R1 is hydrogen or a protecting group; R2 is methyl, ethyl, isopropyl or sec-butyl; and R is a radical R3 which is bound through oxygen or sulfur and is selected from the group consisting of C1-C10alkyl, C1-C10haloalkyl, C1-C10hydroxyalkyl, C1-C10mercaptoalkyl, C2-C10alkoxyalkyl, C3-C10alkoxyalkoxyalkyl, hydroxy- or mercapto-substituted C3-C10alkoxyalkyl, C4-C15alkoxyalkoxyalkoxyalky, hdroxy- or mercapto-substituted C4-C15alkoxyalkoxyalkoxyalkyl, C2-C10-alkenyl, C2-C10haloalkenyl, C2-C10alkynyl, C2-C10haloalkynyl, phenyl which is unsubstituted or substituted by halogen, C1-C3-alkyl, C1-C3haloalkyl, C1-C3alkoxy, C1-C3haloalkoxy, cyano and/or nitro, and benzyl which is unsubstituted or substituted by halogen, C1-C3alkyl, C1-C3haloalkyl, C1-C3alkoxy, C1-C3haloalkoxy, cyano and/or nitro, or R is one of the groups -SH or -S-C(O)OR4, wherein R4 is C1-C10haloalkyl, or a phenyl or benzyl group which is unsubstituted or substituted by halogen, C1-C3alkyl, C1-C3haloalkyl, C1-C3alkoxy, C1-C3haloalkoxy, cyano and/or nitro, and to the preparation thereof starting from suitably substituted 15-hydroxy- or 13 beta -hydroxymilbemycins of formula II.