发明名称 C-8A-OXO-AVERMECTIN AND MILBEMYCIN DERIVATIVES
摘要 Novel avermectin and milbemycin compounds having the formula: …<CHEM>… in which the broken line indicates a single or double bond; R1 is hydrogen, oxo, lower alkanoyloxy, or hydroxy and is present only when the broken line indicates a single bond;… R2 is methyl, ethyl, isopropyl or sec-butyl; R3 is hydroxy, methoxy or lower alkanoyloxy;… R4 is hydrogen, hydroxy, lower alkanoyloxy, alpha -L-oleandrosyloxy, alpha -L-oleandrosyl- alpha -L-oleandrosyloxy, 4 min -loweralkanoyl- alpha -L-oleandrosyloxy, or 4 sec -loweralkonoyl-4 min - alpha -L-oleandrosyl- alpha -L-oleandrosyloxy; or are tri(lower alkyl)silyl protected hydroxy derivatives or pharmaceutically acceptable salts thereof. These compounds are prepared by oxidizing an avermectin or milbemycin compound. They have utility as anti-parasitic agents and may be made into compositions for that use are also disclosed. The compounds are also highly potent insecticides against agricultural pests.
申请公布号 AU4508385(A) 申请公布日期 1986.01.23
申请号 AU19850045083 申请日期 1985.07.17
申请人 MERCK + CO., INC. 发明人 HELMUT M. MROZIK;FRANK S. WAKSMUNSKI
分类号 C07D493/22;A01N43/90;A61K31/365;A61P33/00;C07H17/08;C07H19/01 主分类号 C07D493/22
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