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    • 5. 发明授权
    • Avermectin derivatives
    • 阿维菌素衍生物
    • US06605595B1
    • 2003-08-12
    • US09890824
    • 2002-02-11
    • Satoshi OmuraToshiaki SunazukaAndreas TurbergGeorg von Samson-HimmelstjernaOlaf HansenAchim Harder
    • Satoshi OmuraToshiaki SunazukaAndreas TurbergGeorg von Samson-HimmelstjernaOlaf HansenAchim Harder
    • A01N4304
    • C07H17/08A61K31/7048
    • Avermectin derivatives represented by the general formula (I) or salts thereof: wherein —X----Y— represents —CH═CH—, —CH2—C(═O)—, —CH2—CH2—, or —CH2—CH(R13)—; for example, 1) when —X----Y— represents —CH═CH—, R1 represents (R11)(R12)C [wherein R11 represents a substituted or unsubstituted lower alkyl group; a formyl group; a lower alkoxylcarbonyl group etc.; and R12 represents a hydrogen atom or a lower alkyl group]; when the bond between R2 and a carbon atom at the 5-position is a single bond, R2 represents a hydroxyl group or a tri(lower alkyl)silyloxy group; or R2 forms a carbonyl group or a hydroxime group together with the carbon atom at the 5-position; 2) when —X----Y— represents —CH2—C(═O)—, R1 represents (R11a)(R12a)C [wherein R11a represents a lower alkoxycarbonyl group, or —COOCH2CH═CH2; and R12a represents a hydrogen atom]; and R2 represents a hydroxyl group or a tri(lower alkyl)silyloxy group.
    • 由通式(I)表示的阿维菌素衍生物或其盐:其中-X-Y-表示-CH = CH-,-CH 2 -C(= O) - , - CH 2 -CH 2 - 或-CH 2 - CH(R 13) - ; 例如,1)当-X ----Y-表示-CH = CH-时,R1表示(R11)(R12)C [其中R11表示取代或未取代的低级烷基; 甲酰基; 低级烷氧基羰基等; R12表示氢原子或低级烷基]。 当R 2与5位的碳原子之间的键是单键时,R 2表示羟基或三(低级烷基)甲硅烷氧基; 或R 2与5-位上的碳原子一起形成羰基或羟基基团; 2)当-X ----Y-表示-CH2-C(= O) - 时,R1表示(R11a)(R12a)C [其中R11a表示低级烷氧基羰基或-COOCH2CH = CH2; R12a表示氢原子]; 并且R 2表示羟基或三(低级烷基)甲硅烷氧基。