Radiosynthesis of [^(18)F]ArylSCF2H Using Aryl Boronic Acids, S-(Chlorofluoromethyl) benzenesulfonothioate and [^(18)F]Fluoride  

作　　者：Qunchao Zhao Patrick G.Isenegger Thomas C.Wilson Jeroen BISap Florian Guibbal Long Lu Véronique Gouverneur Qilong Shen 

机构地区：[1]Key Laboratory of Organofluorine Chemistry Center for Excellence in Molecular Synthesis,Shanghai Institute of Organic Chemistry,University of Chinese Academy of Sciences,Chinese Academy of Sciences,Shanghai 200032 [2]Chemistry Research Laboratory,University of Oxford,Oxford OX13TA [3]Shanghai Institute of Organic Chemistry,Chinese Academy of Sciences,Shanghai 200032

出　　处：《CCS Chemistry》2021年第7期1921-1928,共8页中国化学会会刊（英文）

基　　金：support from National Natural Science Foundation of China(nos.21625206,21632009,and 21421002);the Strategic Priority Research Program of the Chinese Academy of Sciences(no.XDB20000000);the Engineering and Physical Sciences Research Council(nos.EP/NP509711/1,EP/L025604/1,and NS/A000024/1);the Biotechnology and Biological Sciences Research Council(no.BB/P026311/1),Pfizer,the Swiss National Science Foundation(no.P2BSP2_178609),and Cancer Research UK(no.C5255/A16466).

摘　　要：Herein,we report a mild and practical protocol for the copper-catalyzed chlorofluoromethylthiolation of(hetero)aryl boronic acids with the novel reagent PhSO2SCFClH.The resulting products are amenable to halogen-exchange^(18)F-fluorination with cyclotronproduced[^(18)F]fluoride affording[^(18)F]ArSCF2H.This process highlights the combined value of reagent development and(hetero)aryl boron precursors for radiochemistry by adding the[^(18)F]SCF2H group to the list of^(18)F-motifs within reach for positron emission tomography studies.

关 键 词：chlorofluoromethylthiolation boron reagent PET FLUORINE RADIOLABELING 

分 类 号：O62[理学—有机化学]