| abstract |
The invention relates to macrolidoa, in particular the preparation of a compound of the general bJOR class, No. N. Where RI is CH3, CaHs or iso-C3H; R2 is lower alkyl and the NOR2 group is in the E-configuration; OH3 is hydroxyl with anthelmintic activity, which can be used in medicine. The goal is the creation of new, more active substances of this class. The synthesis is carried out by oximation of the corresponding ketone, in which the ORz-group can be hydroxyl or protected by hydroxyl, using the compound f-ly II: R2 — H or lower alkyl: R20-NH2, followed by isolation of the target product or, if necessary, sn thiium protective group with hydroxyl-ORcj. In the other case, when Rz1 H and ORa are protected hydroxyl, they are esterified with f-III III: R2 to Y halide. Where Y is halogen, followed by deprotection of hydroxyl. New substances reduce helminth damage to 98% with low toxicity. 2 tab. (L |