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
Amino acids were found to be as good ligands for copper-catalyzed borylation reactions of primary and secondary alkyl halides,and the B2pin2 acted as bi-boron source for borylation.The high reaction efficiency and mil...Amino acids were found to be as good ligands for copper-catalyzed borylation reactions of primary and secondary alkyl halides,and the B2pin2 acted as bi-boron source for borylation.The high reaction efficiency and mild conditions make the new catalyst system a useful alternative to the recently developed methods for the preparation of alkylboronic esters.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.
基金support from the Eastern Scholar,Shanghai Pujiang Program,Key Subject of Shanghai Municipal Education Commission,Natural Science Foundation of Shanghai (No.12ZR1410500)NSFC (Nos.21102088,51202138 and 21174081)
文摘Amino acids were found to be as good ligands for copper-catalyzed borylation reactions of primary and secondary alkyl halides,and the B2pin2 acted as bi-boron source for borylation.The high reaction efficiency and mild conditions make the new catalyst system a useful alternative to the recently developed methods for the preparation of alkylboronic esters.