Nucleophilic fluorination of aromatic compounds
    10.
    发明授权
    Nucleophilic fluorination of aromatic compounds 有权
    芳族化合物的亲核氟化

    公开(公告)号:US08674101B2

    公开(公告)日:2014-03-18

    申请号:US13054458

    申请日:2009-07-13

    IPC分类号: C07D241/18

    摘要: Iodylbenzene derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are used as precursors in aromatic nucleophilic substitution reactions. The iodyl group (IO2) is regiospecifically substituted by nucleophilic fluoride to provide the corresponding fluoroaryl derivatives. No-carrier-added [F-18]fluoride ion derived from anhydrous [F-18](F/Kryptofix, [F-18]CsF or a quaternary ammonium fluoride (e.g., Me4NF, Et4NF, n-Bu4NF, (PhCH2)4NF) exclusively substitutes the iodyl moiety in these derivatives and provides high specific activity F-18 labeled fluoroaryl analogs. Iodyl derivatives of a benzothiazole analog and 6-iodyl-L-dopa derivatives have been synthesized as precursors and have been used in the preparation of no-carrier-added [F-18]fluorobenzothiazole as well as 6-[F-18]fluoro-L-dopa.

    摘要翻译: 在芳香环上使用由电子给体取代的取代基和吸电子基团作为芳族亲核取代反应的前体。 碘基(IO2)被亲核氟化物区域性取代,以提供相应的氟代芳基衍生物。 F-18](F / Kryptofix,[F-18] CsF或季铵氟化物(如Me4NF,Et4NF,n-Bu4NF,(PhCH2))的无载体添加[F-18] 4NF)仅代替这些衍生物中的碘基部分,并提供高比活性F-18标记的氟代芳基类似物。苯并噻唑类似物和6-碘代-L-多巴衍生物的碘代衍生物已被合成为前体,并已用于制备 无载体添加的[F-18]氟代苯并噻唑以及6- [F-18]氟-L-多巴。