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-excha...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.展开更多
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)+1 种基金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).
文摘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.