New automated synthesis of [18F]FP-CIT with base amount control affording high and stable radiochemical yield: a 1.5-year production report.

  title={New automated synthesis of [18F]FP-CIT with base amount control affording high and stable radiochemical yield: a 1.5-year production report.},
  author={S. Lee and S. Oh and Woo Yeon Moon and M. Choi and Jae Seung Kim and D. Chi and D. Moon and J. Ryu},
  journal={Nuclear medicine and biology},
  volume={38 4},
  • S. Lee, S. Oh, +5 authors J. Ryu
  • Published 2011
  • Chemistry, Medicine
  • Nuclear medicine and biology
We describe new [(18)F]Fluoropropylcarbomethoxyiodophenyl-nor-tropane ([(18)F]FP-CIT) automatic preparation method by (1) using 2-methyl-2-butanol as [(18)F]fluorination solvent, (2) base amount control to minimize side reaction and (3) salt elution method to elute trapped [(18)F]fluoride. We developed manual synthesis procedures for automatic synthesis application. In this manual synthesis, we trapped [(18)F]F(-) on ion exchange cartridge and eluted with 0.2 M potassium methanesulfonate… Expand
Development of a new precursor-minimizing base control method and its application for the automated synthesis and SPE purification of [(18) F]fluoromisonidazole ([(18) F]FMISO).
The goal of the current study was to develop a new method for synthesizing radiopharmaceuticals that permits the fine control of base concentrations while minimizing adverse events. Expand
Two-step radiosynthesis of 18)F]FE-β-CIT and [18F]PR04.MZ.
The cocaine-derived dopamine reuptake inhibitors FE-β-CIT and PR04.MZ were obtained after a synthesis time of 100 min in about 25% non-decay-corrected overall yield and 4-[(18)F]fluorobut-2-yne-1-yl tosylate were used as labelling reagents, respectively. Expand
Degradation of acetonitrile in eluent solutions for [18F]fluoride PET chemistry: impact on radiosynthesis of [18F]FACBC and [18F]FDG
In [18F]fluoride chemistry, an eluent solution containing a weak aqueous base is used to release [18F]fluoride after adsorption on an anion exchange resin. Traditionally, the eluent solution isExpand
Full automatic synthesis of [18F]THK-5351 for tau protein PET imaging in Alzheimer’s disease patients: 1 year experience
Abstract[18F]THK-5351, a new candidate for tau protein imaging, is based on an aryl quinoline structure. We report the full automatic synthesis using disposable cassettes under pH controlledExpand
A practical synthesis of [(18) F]FtRGD: an angiogenesis biomarker for PET.
The practical use of the nucleophilic detagging and fluorous solid-phase extraction method for the preparation of the 2-[(18) F]fluoroethyl-triazolyl conjugated c(RGDyK) peptide proved valuable for preclinical positron emission tomography imaging of integrin expression. Expand
High Yielding [ 18 F]Fluorination Method by Fine Control of the Base
F]fluoride is used. To prevent this problem, an exactamount of base must be added to the reactor without appli-cation of an anion exchange cartridge.Direct base addition without an anion exchangeExpand
Organofluorine Compounds as Positron Emission Tomography Tracers
The half-life of the 18 F isotope is the highest among all the positron-emitting isotopes, and therefore positron emission tomography (PET) using 18 F-labeled pharmaceuticals has practical advantageExpand
Feasibility of PET Template-Based Analysis on F-18 FP-CIT PET in Patients with De Novo Parkinson’s Disease
Quantitative parameters using FP-CIT PET template-based method correlated well with those using laborious manual method with excellent concordance, suggesting that PET- based method can provide objective and quantitative parameters quickly and easily as a feasible analysis in place of conventional method. Expand
Dopamine transporter neuroimaging accurately assesses the maturation of dopamine neurons in a preclinical model of Parkinson’s disease
The utility of neuroimaging to characterise the in vivo maturation, innervation and functional dopamine release of transplanted human embryonic stem cell-derived midbrain dopaminergic neurons (hESC-mDAs) in a preclinical model of PD is examined. Expand
Hydrogen-bond promoted nucleophilic fluorination: concept, mechanism and applications in positron emission tomography.
Simultaneous dual activation of reacting partners by intermolecular hydrogen bonding and the enhancement of the "effective fluoride nucleophilicity", which is Nature's biocatalytic approach with the fluorinase enzyme, are the key to this unprecedentedly successful nucleophilic fluorination. Expand


One-step high-radiochemical-yield synthesis of [18F]FP-CIT using a protic solvent system.
The new radiochemistry method using a protic solvent system gave a high radiochemical yield with high reproducibility and might enable [18F]FP-CIT to be used clinically and commercially. Expand
Simple and highly efficient synthesis of 3′-deoxy-3′-[18F]fluorothymidine using nucleophilic fluorination catalyzed by protic solvent
  • S. Lee, S. Oh, +4 authors D. Moon
  • Chemistry, Medicine
  • European Journal of Nuclear Medicine and Molecular Imaging
  • 2007
[18F]FLT was synthesized with a significantly improved radiochemical yield by nucleophilic substitution catalyzed by protic solvent with mild reaction conditions and a short preparation time. Expand
Increased [18F]2-fluoro-2-deoxy-D-glucose ([18F]FDG) yield with recycled target [18O]water: factors affecting the [18F]FDG yield.
  • K. Nishijima, Y. Kuge, +6 authors N. Tamaki
  • Chemistry, Medicine
  • Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine
  • 2002
Levels of several ionic impurities including Cl- and Ca2+ were significantly higher in the virgin [18O]water than in the recycled water, while significantly larger amounts of organic impurities were detected in the former, Hence, trace amounts of organics were not responsible for the lower [18F]FDG yield. Expand
Radiosynthesis of [18F] N-3-fluoropropyl-2-β-carbomethoxy-3-β-(4-iodophenyl) nortropane and the first human study with positron emission tomography
A procedure for the routine preparation of [18F]FP-CIT has been developed. Purification of the final product was achieved by preparative HPLC using phenethyl column without decomposition orExpand
Routine quality control of recycled target [18O]water by capillary electrophoresis and gas chromatography.
The analyses of anions, organics, and isotopic enrichment were applied routinely for quality control of [(18)O]water to predict a satisfactory outcome of 2-[(18)F]FDG production. Expand
Radiosynthesis of [18F] N-(3-Fluoropropyl)-2-β-Carbomethoxy-3-β-(4-Bromophenyl) Nortropane and the regional brain uptake in non human primate using PET
Abstract A synthetic procedure for the preparation of [ 18 F]FPCBT, an imaging agent for the dopamine transporter (DAT), has been developed. The radiosynthesis was carried out in a two stepExpand
A new class of SN2 reactions catalyzed by protic solvents: Facile fluorination for isotopic labeling of diagnostic molecules.
This work introduces a remarkable effect of using tertiary alcohols as a reaction medium for nucleophilic fluorination with alkali metal fluorides, greatly increasing the rate of the nucleophile fluorination and reducing formation of byproducts compared with conventional methods using dipolar aprotic solvents. Expand
[18F]β-CIT-FP is superior to [11C]β-CIT-FP for quantitation of the dopamine transporter
beta-CIT-FP [N-(3-fluoropropyl)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)nortropane] is a cocaine analogue with high affinity for the dopamine transporter. Positron emission tomography (PET) studiesExpand
Investigation of the role of the base in the synthesis of [18F]FLT.
The role of the base in the synthesis of 3'-deoxy-3'-[18F]fluorothymidine, [18F]FLT, via nucleophilic substitution of the nosyl group with [18F]fluoride was investigated. The rate ofExpand
Dopamine transporter imaging with fluorine-18-FPCIT and PET.
FPCIT/PET demonstrated age-related decline in dopamine transporter binding in normal subjects as well as significant reductions in patients with idiopathic Parkinson's disease, which correlates with the disease severity. Expand