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增强的铜介导的芳基硼酸酯的(18)F氟化反应为正电子发射断层扫描(PET)应用提供了八种放射性示踪剂。

Enhanced copper-mediated (18)F-fluorination of aryl boronic esters provides eight radiotracers for PET applications.

作者信息

Preshlock Sean, Calderwood Samuel, Verhoog Stefan, Tredwell Matthew, Huiban Mickael, Hienzsch Antje, Gruber Stefan, Wilson Thomas C, Taylor Nicholas J, Cailly Thomas, Schedler Michael, Collier Thomas Lee, Passchier Jan, Smits René, Mollitor Jan, Hoepping Alexander, Mueller Marco, Genicot Christophe, Mercier Joël, Gouverneur Véronique

机构信息

University of Oxford, Chemistry Research Laboratory, 12 Mansfield Road, OX1 3TA Oxford, UK.

Imanova, Burlington Danes building Imperial College, London Hammersmith Hospital, Du Cane Road, London W12 0NN, UK.

出版信息

Chem Commun (Camb). 2016 Jun 28;52(54):8361-4. doi: 10.1039/c6cc03295h.

Abstract

[(18)F]FMTEB, [(18)F]FPEB, [(18)F]flumazenil, [(18)F]DAA1106, [(18)F]MFBG, [(18)F]FDOPA, [(18)F]FMT and [(18)F]FDA are prepared from the corresponding arylboronic esters and [(18)F]KF/K222 in the presence of Cu(OTf)2py4. The method was successfully applied using three radiosynthetic platforms, and up to 26 GBq of non-carrier added starting activity of (18)F-fluoride.

摘要

[(18)F]FMTEB、[(18)F]FPEB、[(18)F]氟马西尼、[(18)F]DAA1106、[(18)F]MFBG、[(18)F]FDOPA、[(18)F]FMT和[(18)F]FDA是在Cu(OTf)2py4存在下由相应的芳基硼酸酯和[(18)F]KF/K222制备而成。该方法已成功应用于三个放射性合成平台,起始活度高达26 GBq的无载体添加(18)F-氟化物。

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