Process of producing 8A- and 9A-azalide antibiotics
    4.
    发明授权
    Process of producing 8A- and 9A-azalide antibiotics 失效
    生产8A-和9A-氮杂抗生素的方法

    公开(公告)号:US5332807A

    公开(公告)日:1994-07-26

    申请号:US48048

    申请日:1993-04-14

    CPC分类号: C07H17/02 C07H17/00

    摘要: A process of producing 8a- and 9a- azalide compounds is disclosed, comprised of reacting an 8a- aza or 9a- aza azalide eastern fragment or a derivative thereof with a compound of the formula:X--A'--Ywherein X and Y are appropriate reactive groups and A' is a fragment or compound which forms the western portion of the azalide, andcyclizing this intermediate to form the target 8a- or 9a-azalide compound. Compounds of formula I, II and III as well as other azalides can be synthesized according to this process.

    摘要翻译: 公开了一种制备8α和9α-氮杂化合物的方法,其包括使8-氮杂或9-氮杂氮杂东片段或其衍生物与下式化合物:X-A'-Y反应,其中X和Y为 合适的反应性基团和A'是形成氮杂环化合物的西部的片段或化合物,并使该中间体环化以形成目标8a-或9a-氮杂化合物。 式I,II和III的化合物以及其它的氮杂化物可以根据该方法合成。

    Synthetic marcfortine derivatives useful as antiparasitic agents
    10.
    发明授权
    Synthetic marcfortine derivatives useful as antiparasitic agents 失效
    用作抗寄生虫剂的合成马可氟汀衍生物

    公开(公告)号:US4923867A

    公开(公告)日:1990-05-08

    申请号:US235418

    申请日:1988-08-24

    IPC分类号: A01N43/90 C07D491/22

    CPC分类号: C07D491/22 A01N43/90

    摘要: There are disclosed synthetic marcfortine derivatives of the natural products marcfortine A, marcfortine B, and marcfortine C. The synthetic derivatives are described in the following formula: ##STR1## wherein: n is 0 or 1R.sub.1 is hydrogen, loweralkyl, benzyl, lower alkanoyl, benzenesulfonyl in which the benzene ring is substituted with from 0 to 3 substituents selected from lower alkyl groups, lower alkoxy groups and halogen atoms, lower alkylamino-carbonyl, lower alkoxy-carbonyl;R.sub.24 is hydrogen, halogen or lower alkoxy (provided that R.sub.24 is other than hydrogen only if the broken line represents a single bond at the 24, 25-position),R.sub.25 is hydrogen or halogen (provided that R.sub.25 is other than hydrogen only if the broken line represents a single bond at the 24, 25-position);R.sub.29 is hydrogen, lower alkyl, alkoxyalkyl, haloalkyl, lower alkenyl, lower alkynyl, benzyl, lower alkanoyl, substituted benzenesulfonyl, lower alkylamino-carbonyl, not hydrogen or methyl if R.sub.1 is hydrogen; and the broken line represents a single or double bond between carbons 24 and 25.The compounds are active antiparasitic agents useful in particular against insect and nematode pests, and compositions for that use are disclosed.

    摘要翻译: 公开了天然产物马可氟汀A,马可氟汀B和马可氟汀C的合成马可氟汀衍生物。合成衍生物描述于下式中:其中:n为0或1,R1为氢,低级烷基,苄基,低级烷酰基 苯磺酰基,其中苯环被0-3个选自低级烷基,低级烷氧基和卤素原子的取代基取代,低级烷基氨基 - 羰基,低级烷氧羰基; R24是氢,卤素或低级烷氧基(只要虚线表示24,25位的单键,R24不是氢),R25是氢或卤素(只要R25不是氢,只要是 虚线代表24,25位的单键); 如果R1是氢,R29是氢,低级烷基,烷氧基烷基,卤代烷基,低级烯基,低级炔基,苄基,低级烷酰基,取代的苯磺酰基,低级烷基氨基 - 羰基,不是氢或甲基; 并且虚线表示碳24和25之间的单键或双键。化合物是有效的抗寄生虫剂,特别适用于昆虫和线虫害虫,并且公开了该用途的组合物。