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    • 15. 发明专利
    • 5-oxime derivative of milbemycins
    • 5-OXIME MILBEMYCINS衍生物
    • JPS59108785A
    • 1984-06-23
    • JP20646282
    • 1982-11-25
    • Sankyo Co Ltd
    • IDE JIYUNYAMURAMATSU SHIGEKINAKADA YASUOKITANO KUNITOSHI
    • C07H15/238A01N43/90A01N63/02A61K31/35A61P33/00C07D493/22C07H19/01
    • C07H19/01A01N43/90
    • NEW MATERIAL:The didehydromilbemycin 5-oxime derivative of formula I [R
      1 is methyl, ethyl or i-propyl; the bond between 3 and 4 sites containing the dotted line is single or double; when the bond between 3 and 4 sites is double, R
      2 is H, and when it is single, R
      2 is H or -NHOR
      3 (R
      3 is H or methyl); R
      3 in the formula I is H, lower alkyl or aralkyl] and its salt.
      EXAMPLE: 5-Didehydromilbemycin D 5-oxime (A) and 3,4-dihydro-3-hydroxyamino- 5-didehydromilbemycin D 5-oxime (B).
      USE: Miticide and anthelminitic.
      PROCESS: The compound of formula I can be prepared by reacting the compound of formula II with the oximation agent of formula NH
      2 OR
      3 in an inert solvent preferably in the presence of a base (e.g. triethylamine, pyridine, etc.) at -10W +100°C for 0.5W10hr, preferably at 0W50°C for 1W5hr.
      COPYRIGHT: (C)1984,JPO&Japio
    • 新物质:式I的脱氢吗啉霉素5-肟衍生物[R1是甲基,乙基或异丙基; 包含虚线的3至4个位点之间的键是单或双; 当3和4位之间的键是双重的时,R2是H,当它是单键时,R2是H或-NHOR3(R3是H或甲基); 式I中的R 3是H,低级烷基或芳烷基]及其盐。 实施例:5-二脱水霉素D 5 - 肟(A)和3,4-二氢-3-羟基氨基-5-二脱水吗啉霉素D 5 - 肟(B)。 使用:杀螨剂和anthelminitic。 方法:式I化合物可以通过使式II化合物与式NH 2 OR 3的肟化剂在惰性溶剂中反应来制备,优选在-10〜+100的碱(例如三乙胺,吡啶等)存在下, 摄氏0.5-10小时,优选0-50摄氏度1-5小时。