No-carrier-added (NCA) aryl (18E) fluorides via the nucleophilic
aromatic substitution of electron rich aromatic rings
    12.
    发明授权
    No-carrier-added (NCA) aryl (18E) fluorides via the nucleophilic aromatic substitution of electron rich aromatic rings 失效
    无载体添加(NCA)芳基(18E)氟化物通过富含芳族芳环的亲核芳烃取代

    公开(公告)号:US5254726A

    公开(公告)日:1993-10-19

    申请号:US711684

    申请日:1991-06-07

    摘要: A method for synthesizing no-carrier-added (NCA) aryl [.sup.18 F] fluoride substituted aromatic aldehyde compositions bearing an electron donating group is described. The method of the present invention includes the step of reacting aromatic nitro aldehydes having a suitably protected hydroxyl substitutent on an electron rich ring. The reaction isThe U.S. Government has rights in this invention pursuant to Contract Number DE-AC02-76CH00016, between the U.S. Department of Energy and Associated Universities Inc.

    摘要翻译: 描述了一种合成具有给电子基团的无载体添加(NCA)芳基[18 F]氟取代的芳族醛组合物的方法。 本发明的方法包括使具有适当保护的羟基取代基的芳族硝基醛与富电子环反应的步骤。 该反应通过亲核芳族取代通过无载体添加(NCA)[18F]氟离子进行。 本发明的方法可用于合成各种无载体添加的芳基[18 F]氟化物组合物,包括6- [18 F]氟-L-多巴,2- [18 F]氟酪氨酸,6- [18 F]氟去甲肾上腺素, 和6- [18F]氟代多巴胺。 在通过本发明产生对映异构体的外消旋混合物的情况下,例如在6- [18 F]氟去甲肾上腺素的合成中,优选的方法还包括在手性HPLC柱上拆分外消旋混合物。 该方法导致高产率的对映体纯的[18 F]标记的异构体,例如[ - ] - 6- [18 F]氟去甲肾上腺素和[+] - 6- [18F]氟去甲肾上腺素。

    No-carrier-added [1.sup.11 c]putrescine
    13.
    发明授权
    No-carrier-added [1.sup.11 c]putrescine 失效
    无载体添加[111c]腐胺

    公开(公告)号:US4874600A

    公开(公告)日:1989-10-17

    申请号:US853105

    申请日:1986-04-17

    IPC分类号: A61K51/04

    CPC分类号: A61K51/0406 A61K2123/00

    摘要: The invention relates to a new radiolabeled imaging agent, no-carrier-added [1-.sup.11 C]putrescine, and to the use of this very pure material as a radiotracer with positron emission tomography for imaging brain tumors. The invention further relates to the synthesis of no-carrier-added [1-.sup.11 C]putrescine based on the Michael addition of potassium .sup.11 C-labeled cyanide to acrylonitrile followed by reduction of the .sup.11 C-labeled dinitrile. The new method is rapid and efficient and provides radiotracer with a specific activity greater than 1.4 curies per millimol and in a purity greater than 95%.

    摘要翻译: 本发明涉及一种新的放射性标记成像剂,无载体添加的[1-11C]腐胺,以及使用这种非常纯的材料作为放射性示踪剂,具有用于成像脑肿瘤的正电子发射断层扫描。 本发明还涉及基于将11C标记的氰化钾向丙烯腈中迈克尔加成,然后还原11C-标记的二腈,合成无载体添加的[1-11C]腐胺。 新方法快速有效,并提供具有大于1.4百分点/毫摩尔的比活性的放射性示踪剂,纯度大于95%。