Reactions of cyclotron-produced [18F]fluoride with diaryliodonium salts—a novel single-step route to no-carrier-added [18]fluoroarenes

Author(s):  
Victor W. Pike ◽  
Franklin I. Aigbirhio
2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Nashaat Turkman ◽  
Daxing Liu ◽  
Isabella Pirola

AbstractSmall molecules that contain the (TFMO) moiety were reported to specifically inhibit the class-IIa histone deacetylases (HDACs), an important target in cancer and the disorders of the central nervous system (CNS). However, radiolabeling methods to incorporate the [18F]fluoride into the TFMO moiety are lacking. Herein, we report a novel late-stage incorporation of [18F]fluoride into the TFMO moiety in a single radiochemical step. In this approach the bromodifluoromethyl-1,2,4-oxadiazole was converted into [18F]TFMO via no-carrier-added bromine-[18F]fluoride exchange in a single step, thus producing the PET tracers with acceptable radiochemical yield (3–5%), high radiochemical purity (> 98%) and moderate molar activity of 0.33–0.49 GBq/umol (8.9–13.4 mCi/umol). We validated the utility of the novel radiochemical design by the radiosynthesis of [18F]TMP195, which is a known TFMO containing potent inhibitor of class-IIa HDACs.


2015 ◽  
Vol 81 (1) ◽  
pp. 297-302 ◽  
Author(s):  
Mohammad B. Haskali ◽  
Sanjay Telu ◽  
Yong-Sok Lee ◽  
Cheryl L. Morse ◽  
Shuiyu Lu ◽  
...  

2007 ◽  
Vol 129 (25) ◽  
pp. 8018-8025 ◽  
Author(s):  
Tobias L. Ross ◽  
Johannes Ermert ◽  
Carsten Hocke ◽  
Heinz H. Coenen

2019 ◽  
Vol 55 (75) ◽  
pp. 11267-11270 ◽  
Author(s):  
Shiqing Li ◽  
Hongxu Lv ◽  
Yu Yu ◽  
Xiuqing Ye ◽  
Baisong Li ◽  
...  

A Cu-mediated domino di-/triarylation reaction of imidazoles in a single step by using two aryls as well as an anion of a diaryliodonium salt is developed to quickly achieve polyaryl imidazolium salts.


2010 ◽  
Vol 122 (18) ◽  
pp. 3229-3232 ◽  
Author(s):  
Christian F. Lemaire ◽  
Joël J. Aerts ◽  
Samuel Voccia ◽  
Lionel C. Libert ◽  
Frédéric Mercier ◽  
...  

2010 ◽  
Vol 68 (9) ◽  
pp. 1703-1708 ◽  
Author(s):  
Hidekazu Saiki ◽  
Ren Iwata ◽  
Hiroaki Nakanishi ◽  
Rebecca Wong ◽  
Yoichi Ishikawa ◽  
...  

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