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    • 3. 发明授权
    • Process for producing pyripyropene derivatives and intermediates for the production thereof
    • 生产拟南芥衍生物的方法及其生产用中间体
    • US08263778B2
    • 2012-09-11
    • US12733113
    • 2008-08-13
    • Kimihiko GotoKazumi YamamotoMasayo SakaiMasaaki MitomiTakashi Ando
    • Kimihiko GotoKazumi YamamotoMasayo SakaiMasaaki MitomiTakashi Ando
    • C07D493/04
    • C07D493/04Y02P20/55
    • Disclosed is a process for producing compound C represented by formula C: wherein R′ represents straight chain, branched chain, or cyclic C2-6 alkylcarbonyl, wherein R1b is used as a protective group for hydroxyl at the 7-position of compound C. R1b represents formyl; optionally substituted straight chain C1-4 alkylcarbonyl; optionally substituted benzyl; group —SiR3R4R5 optionally substituted by halogen atom wherein R3, R4, and R5 each independently represent straight chain or branched chain C1-6 alkyl or phenyl; C1-6 alkyloxy-C1-6 alkyl optionally substituted by halogen atom; C1-6 alkylthio-C1-6 alkyl optionally substituted by halogen atom; straight chain, branched chain, or cyclic C1-4 alkyl optionally substituted by halogen atom, provided that, when alkyl in the C1-4 alkyl group is of a branched chain or cyclic type, the alkyl group is C3-4 alkyl; C2-6 alkenyl optionally substituted by halogen atom; C2-6 alkynyl optionally substituted by halogen atom; or an optionally substituted saturated or unsaturated five- or six-membered heterocyclic group. The process can produce pyripyropene derivatives that have acyloxy groups at the 1- and 11-positions and a hydroxyl group at the 7-position and are useful as insect pest control agents at a high yield.
    • 公开了一种制备由式C表示的化合物C的方法:其中R'表示直链,支链或环状C 2-6烷基羰基,其中R 1b用作化合物C的7-位羟基保护基。R1b 代表甲酰基; 任选取代的直链C 1-4烷基羰基; 任选取代的苄基; 基团-SiR 3 R 4 R 5任选被卤素原子取代,其中R 3,R 4和R 5各自独立地表示直链或支链C 1-6烷基或苯基; 任选被卤素原子取代的C 1-6烷氧基-C 1-6烷基; 任选被卤素原子取代的C 1-6烷硫基-C 1-6烷基; 直链,支链或任选被卤素原子取代的环状C 1-4烷基,条件是当C 1-4烷基中的烷基为支链或环状时,该烷基为C 3-4烷基; 任选被卤素原子取代的C 2-6烯基; 任选被卤素原子取代的C 2-6炔基; 或任选取代的饱和或不饱和的五元或六元杂环基。 该方法可以产生在1-位和11位上具有酰氧基并且在7-位上具有羟基并且以高产率用作害虫控制剂的吡哆烯衍生物。