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    1,2,3-트리아졸기를 갖는 새로운 말레이미드 화합물, 이의 제조방법 및 이를 보결그룹으로 하는 생체화합물의 Ｆ­18 표지방법
    1.
    发明公开
    1,2,3-트리아졸기를 갖는 새로운 말레이미드 화합물, 이의 제조방법 및 이를 보결그룹으로 하는 생체화합물의 Ｆ­18 표지방법 有权
    具有1,2,3-三唑基的新型马来酰亚胺化合物，其制备方法和F-18使用预聚物的生物分子的标记方法

    公开(公告)号：KR1020110131022A

    公开(公告)日：2011-12-06

    申请号：KR1020100050628

    申请日：2010-05-28

    Applicant: 서강대학교산학협력단

    Inventor： 지대윤 ,  이병세 ,  이보람 ,  추소영 ,  이상주

    IPC: C07D403/04 ,  C07D403/02 ,  G01N33/58

    Abstract: PURPOSE: A maleimide compound labeled with fluorine-18(^18F) and a method for labeling ^18F of biocompounds are provided to simplify production process and to reduce production time. CONSTITUTION: A maleimide compound with 1,2,3-triazole group is denoted by chemical formula 1. A method for preparing the maleimide compound comprises: a step of performing nucleophilic fluorination of sulfonate precursor of chemical formula 2 under the presence of an organic solvent to prepare fluoroalkyl azide compound of chemical formula 3; and a step of reacting the compound of chemical formula 3 with maleimide with terminal alkyne group of chemical formula 4 under the presence of an organic solvent and copper catalyst to prepare a compound of chemical formula 1. A method for labeling ^18F to a biocompound comprises: a step of stirring ^18F-labeled compound of chemical formula 1 with the biocompound with SH functional groups under the presence of PBS solution; and a step of collecting ^18F-labeled biocompound of chemical formula 6.

    Abstract translation: 目的：提供用氟-18（^ 18F）标记的马来酰亚胺化合物和用于标记生物化合物的18 F的方法，以简化生产过程并缩短生产时间。 构成：具有1,2,3-三唑基的马来酰亚胺化合物由化学式1表示。马来酰亚胺化合物的制备方法包括：在有机溶剂存在下进行化学式2的磺酸酯前体的亲核氟化的步骤 制备化学式3的氟烷基叠氮化合物; 以及在有机溶剂和铜催化剂的存在下使化学式3的化合物与马来酰亚胺与化学式4的末端炔基反应以制备化学式1的化合物的步骤。将生物化合物标记为18 F的方法包括 ：在PBS溶液存在下，用SH官能团将生物化合物与化学式1化合物的18 F标记化合物进行搅拌; 并收集化学式6的^ 18F标记的生物化合物的步骤。

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