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    • 4. 发明公开
    • 1,2,3-트리아졸기를 갖는 설포네이트 전구체, 이의 제조방법 및 이의 응용
    • 具有1,2,3-三唑基团的磺酸盐前体,其制备和应用
    • KR1020110130977A
    • 2011-12-06
    • KR1020100050565
    • 2010-05-28
    • 서강대학교산학협력단
    • 지대윤이병세권혜림추소영
    • C07D249/04C07D405/12A61K49/00
    • Y02P20/55C07D249/04A61K51/0453C07D403/12
    • PURPOSE: A method for preparing a sulfonate precursor with 1,2,3-triazole group is provided to manufacture [^18F]radioactive chemical. CONSTITUTION: A sulfonate compound with 1,2,3-triazole group is denoted by chemical formula 1. A method for preparing the sulfonate compound comprises: a step of reacting azidoalkanesufonyl chloride of chemical formula 3 with an aliphatic alcohol functional group of chemical formula 4 under the presence of organic solvent and base to prepare an azidoalkane sulfonate compound of chemical formula 5; and a step of reacting the compound of chemical formula 5 with terminal alkyne functional group of chemical formula 6 under the presence of organic solvent and copper catalyst. The base is bicarbonate ion, carbonate ion, alkali metal salt, triethylamine, diisopropylethylamine, pyridine, lutidine, and collidine.
    • 目的:制备具有1,2,3-三唑基团的磺酸酯前体的方法,以制备[^ 18F]放射性化学品。 构成:具有1,2,3-三唑基的磺酸酯化合物由化学式1表示。制备磺酸酯化合物的方法包括:使化学式3的叠氮基烷基磺酰氯与化学式4的脂族醇官能团反应的步骤 在有机溶剂和碱的存在下,制备化学式5的叠氮烷基磺酸酯化合物; 以及在有机溶剂和铜催化剂存在下使化学式5的化合物与化学式6的末端炔官能团反应的步骤。 碱是碳酸氢根离子,碳酸根离子,碱金属盐,三乙胺,二异丙基乙胺,吡啶,二甲基吡啶和可力丁。