Synthesis, radiosynthesis, and positron emission tomography neuroimaging using 5‐[¹⁸F]fluoro‐L‐amino suberate

Abstract

System xc‐ (Sxc‐) has emerged as a new biological target for PET studies to detect oxidative and excitotoxic stress. Notably, applications have, thus far, been limited to tumour imaging although Sxc‐) may play a major role in neurodegeneration. The synthesis procedures of tosylate precursor and its translation to Sxc‐ PET tracer 5[18F]fluoro‐L‐amino suberate by manual and automated radiosyntheses are described. A brain‐PET study has been conducted to evaluate the tracer uptake into brain in healthy mice.

Enzymatic synthesis of fluorinated compounds

“…This ( 18 F-DOPA) PET could be applied to assess the volume of remaining gliomas in the patient, Parkinson's syndrome, and focal hyperinsulinemia in infants, which was a perfect complement to the traditional detection technology. Except that, other types of fluorinated compounds were also used as PET tracers for cancer and tumor detection, such as 18 F-PSMA-1007 (Dietlein et al 2020 ), l -2- 18 F-FAMP, d -2/3/4- 18 F-FAMP and l -3- 18 F-FAMT (Hanaoka et al 2019 ; Mahendra et al 2020 ; Shimizu et al 2019 ), ( 18 F-FBPA) (Romanov et al 2020 ), 18 F-fluoro-ethyl- l -tyrosine ( 18 F-FET) (Fuenfgeld et al 2020 ; Marner et al 2019 ), 6- 18 F-fluoro-meta-tyrosine ( 18 F-FMT) (Badin et al 2019 ; Kojima et al 2019 ; Miyamoto et al 2020 ), N -[ 18 F]-fluoropropylJDTic (Schmitt et al 2017 ), 2-(3-(1-carboxy-5-[(6- 18 F-fluoro-pyridine-3-carbonyl)-amino]-pentyl)-ureido)-pentanedioic acid ( 18 F-DCFPyL) (Jansen et al 2019 ; Rousseau et al 2019 ; Rowe et al 2020a , 2020b ), 5- 18 F-fluoro- l -amino suberate ( 18 F-FASu) (Alluri et al 2020 ; Colovic et al 2019 ), 4-borono-2- 18 F-fluoro- l -phenylalanine fluorine substituted 3-azabicyclo hexane (Chen et al 2019b ), and [ 18 F]FDA-PEG-biotin/tetrazine (Lowe et al 2018 ). Therefore, PET tracers based on new fluorinated compounds will play an increasing role in the field of visual detection technology.…”