• Title/Summary/Keyword: Fluorine-18

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Organometallic fluorine-18 bonds in 18F-radiochemistry

  • Joong-Hyun Chun;Minju Lee;Sungwon Jun;Jeongmin Son
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.7 no.1
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    • pp.22-32
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    • 2021
  • Fluorine-18 is by far the most widely exploited radionuclide in PET (positron emission tomography) radiochemistry. The physical half-life of fluorine-18 allows for chemical manipulation within a restricted timeframe, and cyclotron-produced fluoride ion has been widely applied in aliphatic and aromatic nucleophilic radiofluorinations to produce a variety of established radiotracers. Radiotracers have become more structurally complicated to address diverse targets in physiobiological systems. There is therefore an unmet need to complement traditional C-18F bond-forming radiofluorination with new and efficient radiolabeling techniques to tackle the myriad of possible chemical environments. This review discusses recent advances in organometallic fluorine-18 bond creation in 18F-radiochemistry. Although not widely employed, new radiolabeling strategies for constructing boron-18F, silicon-18F, aluminum-18F, and other metal-18F bonds are described in view of their potential use in the development of novel radiopharmaceuticals.

A Review on the Analytical Techniques for the Determination of Fluorine Contents in Soil and Solid Phase Samples (토양 및 고체시료 중 불소함량 측정기법)

  • An, Jinsung;Kim, Joo-Ae;Yoon, Hye-On
    • Journal of Soil and Groundwater Environment
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    • v.18 no.1
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    • pp.112-122
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    • 2013
  • Current status of soil contamination with fluorine and its source were investigated. The basic principles and procedures of various techniques for the analysis of fluorine contents in soil and solid phase samples were summarized in this review. Analysis of fluorine in solid matrices can be achieved by two types of techniques: (i) UV/Vis spectrophotometer or ion selective electrode (ISE) analysis after performing appropriate extraction steps and (ii) direct solid analysis. As the former cases, the standard method of Korean ministry of environment, alkali fusion-ISE method, pyrohydrolysis, oxygen bomb combustion, aqua regia digestion-automatic analysis, and sequential extraction-ISE method were introduced. In addition, direct analysis methods (i.e., X-ray fluorescence spectrometry and proton induced gamma-ray emission spectrometry) and atomic spectrometry combining with the equipment for introducing solid phase sample were also reviewed. Fluorine analysis techniques can be reasonably selected through site-specific information such as matrix condition, contamination level, the amount of samples and the principles of various methods for the analysis of fluorine presented in this review.

Nucleophilic Fluorination Reactions in Novel Reaction Media for $^{18}F$-Fluorine Labeling Method ($^{18}F$-플루오린 표지를 위한 신개념 반응용매에서 친핵성 불소화 반응)

  • Kim, Dong-Wook;Jeong, Hwan-Jeong;Lim, Seok-Tae;Sohn, Myung-Hee
    • Nuclear Medicine and Molecular Imaging
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    • v.43 no.2
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    • pp.91-99
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    • 2009
  • Noninvasive imaging of molecular and biological processes in living subjects with positron emission tomography(PET) provides exciting opportunities to monitor metabolism and detect diseases in humans. Measuring these processes with PET requires the preparation of specific molecular imaging probes labeled with $^{18}F$-fluorine. In this review we describe recent methods and novel trends for the introduction of $^{18}F$-fluorine into molecules which in turn are intended to serve as imaging agents for PET study. Nucleophilic $^{18}F$-fluorination of some halo- and mesyloxyalkanes to the corresponding $^{18}F$-fluoroalkanes with $^{18}F$-fluoride obtained from an $^{18}O(p,n)^{18}F$ reaction, using novel reaction media system such as an ionic liquidor tert-alcohol, has been studied as a new method for $^{18}F$-fluorine labeling. Ionic liquid method is rapid and particularly convenient because $^{18}F$-fluoride in $H_2O$ can be added directly to the reaction media, obviating the careful drying that is typically required for currently used radiofluorination methods. The nonpolar protic tert-alcohol enhances the nucleophilicity of the fluoride ion dramatically in the absence of any kind of catalyst, greatly increasing the rate of the nucleophilic fluorination and reducing formation of byproducts compared with conventional methods using dipolar aprotic solvents. The great efficacy of this method is a particular advantage in labeling radiopharmaceuticals with $^{18}F$-fluorine for PETimaging, and it is illustrated by the synthesis of $^{18}F$-fluoride radiolabeled molecular imaging probes, such as $^{18}F$-FDG, $^{18}F$-FLT, $^{18}F$-FP-CIT, and $^{18}F$-FMISO, in high yield and purity and in shorter times compared to conventional syntheses.

A Novel Aromatic Fluorine-18 Labeling Method Using Iodonium Salts Precursor (이오도늄 솔트 전구체를 이용한 새로운 방향족 화합물 플루오린-18 표지 기술)

  • Moon, Byung-Seok;Lee, Byung-Chul;Kim, Sang-Eun
    • Nuclear Medicine and Molecular Imaging
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    • v.43 no.1
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    • pp.1-9
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    • 2009
  • As many new drug substances contained various aromatic rings and fluorine attached to an electron rich aromatic ring or on the meta-position, a strategy towards improvement in aromatic fluorination of these compounds is highly desirable. The introduction of fluorine-18 onto aromatic rings showed in the limited condition containing electron withdrawing group (EWG) on the para- or ortho-position to get reasonable radiochemical yield so far. No-carrier added (NCA) [$^{18}F$]fluoroarene syntheses by iodonium salts recently reported that has the potential to greatly increase the yield in systems or positions that normally not reactive enough to give sufficient yields in simple model reaction. This review describes the methodological approach towards effective aromatic fluorination by diaryliodonium salts and future prospects in an application of novel PET radiotracer.

Oral Health Conditions of College Students in Some Regions Based on Fluorine Awareness (대학생의 불소인식도에 따른 구강건강상태)

  • Yoon, Sung-Uk;Oh, Na-Rae;Kim, Jeong-Sun
    • The Journal of the Korea Contents Association
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    • v.15 no.11
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    • pp.329-337
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    • 2015
  • Fluorine is an element that promotes dental caries preventive effect at proper concentration level, but may have significantly undesirable impact on dental caries if correct information of fluorine is not recognized. Therefore, this study is intended to evaluate fluorine awareness among the adults in their 20s and analyze oral health conditions based on such awareness in order to promote dental caries preventive effect and convey correct knowledge of fluorine. For this study, 82 adult men and 102 adult women in their 20s, all of whom lived in Daegu, Gyeongsangbuk-do, were surveyed from May 1, 2014 to June 30 of the same year, along with oral health examination to evaluate their oral health conditions. The results of the analysis showed that 19.46% of respondents answered "No" to the question related to awareness towards the use of fluorine in DT rate dental clinic based on the degree of fluorine awareness, which was higher than 11.10% who answered "Yes"(p<.05). Moreover, 18.32%of respondents answered "No" to the question related to whether they were checking the label indicating the fluorine content in product, which was the highest rate, suggesting that the rate was higher when there was stronger tendency to avoid reading the precaution notice (p<.05). In addition, 71.98% of respondents answered "Yes" to the question associated with the awareness to the use of fluorine in FT rate dental clinic based on the fluorine awareness, which was higher than 49.04% of respondents who answered "No" (p<.05). This study is meaningful in that it provides basic data for the implementation of fluorine prevention projects in the period ahead by determining the effect of fluorine awareness on oral health conditions. Based on aforesaid results, both educational and promotional activities need to be carried out vigorously to help raise fluorine awareness.

Production of $[^{18}F]F_2$ Gas for Electrophilic Substitution Reaction (친전자성 치환반응을 위한 $[^{18}F]F_2$ Gas의 생산 연구)

  • Moon, Byung-Seok;Kim, Jae-Hong;Lee, Kyo-Chul;An, Gwang-Il;Cheon, Gi-Jeong;Chun, Kwon-Soo
    • Nuclear Medicine and Molecular Imaging
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    • v.40 no.4
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    • pp.228-232
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    • 2006
  • Purpose: electrophilic $^{18}F(T_{1/2}=110\;min)$ radionuclide in the form of $[^{18}F]F_2$ gas is of great significance for labeling radiopharmaceuticals for positron omission tomography (PET). However, its production In high yield and with high specific radioactivity is still a challenge to overcome several problems on targetry. The aim of the present study was to develop a method suitable for the routine production of $[^{18}F]F_2$ for the electrophilic substitution reaction. Materials and Methods: The target was designed water-cooled aluminum target chamber system with a conical bore shape. Production of the elemental fluorine was carried out via the $^{18}O(p,n)^{18}F$ reaction using a two-step irradiation protocol. In the first irradiation, the target filled with highly enriched $^{18}O_2$ was irradiated with protons for $^{18}F$ production, which were adsorbed on the inner surface of target body. In the second irradiation, the mixed gas ($1%[^{19}F]F_2/Ar$) was leaded into the target chamber, fellowing a short irradiation of proton for isotopic exchange between the carrier-fluorine and the radiofluorine absorbed in the target chamber. Optimization of production was performed as the function of irradiation time, the beam current and $^{18}O_2$ loading pressure. Results: Production runs was performed under the following optimum conditions: The 1st irradiation for the nuclear reaction (15.0 bar of 97% enriched $^{18}O_2$, 13.2 MeV protons, 30 ${\mu}A$, 60-90 min irradiation), the recovery of enriched oxygen via cryogenic pumping; The 2nd irradiation for the recovery of absorbed radiofluorine (12.0 bar of 1% $[^{19}F]fluorine/argon$ gas, 13.2 MeV protons, 30 ${\mu}A$, 20-30 min irradiation) the recovery of $[^{18}F]fluorine$ for synthesis. The yield of $[^{18}F]fluorine$ at EOB (end of bombardment) was achieved around $34{\pm}6.0$ GBq (n>10). Conclusion: The production of $^{18}F$ electrophilic agent via $^{18}O(p,n)^{18}F$ reaction was much under investigation. Especially, an aluminum gas target was very advantageous for routine production of $[^{18}F]fluorine$. These results suggest the possibility to use $[^{18}F]F_2$ gas as a electrophilic substitution agent.

A STUDY ON THE TRANSFER OF RADIOACTIVE FLUORINE (18F) TO DENTAL HARD TISSUE (방사성(放射性) 불소(弗素)(18F)의 치아경조직내(齒牙硬組織內) 침투(浸透)에 관(關)한 실험적(實驗的) 연구(硏究))

  • Oh, An-Min
    • Restorative Dentistry and Endodontics
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    • v.2 no.1
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    • pp.15-19
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    • 1976
  • The author studied on the transfer of radioactive fluorine ($^{18}F$) to dental hard tissue through animal experiments which was divided into two groups. First group of rats were sacrified 1, 2, 5, 10 and 20 minutes after intraperitoneal injection. Second group were sacrified 1 and 3 minutes after topical application on anterior teeth. The teeth were removed and sectioned by means of abrasive wheel and polished on india stone as thick as about 50 microns. Autoradiograph picture was made by close contact of high-speed dental X-ray film on prepared specimen for 2 hours. The results of this study were as follows; 1) There was no evidence of transfer of $^{18}F$ on dental hard tissue on the cases of 1, 2 and 5 minutes survival after intraperitoneal injection. 2) Radioactive sodium fluorine incorporated to dental hard tissue was slight and diffuse at 10 minutes cases and significant incorporated picture was noticed at 20 minutes cases in intraperitoneal injection. 3) On topical application groups incorporated $^{18}F$ to enamel was traced clearly only on enamel surface at 1 minute cases and significant transfer into whole enamel was found at 3 minutes cases.

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Evaluation of PET Image for Fluorine-18 and Gallium-68 using Phantom in PET/CT (PET/CT에서 Phantom을 이용한 Fluorine-18, Gallium-68 방사성 핵종의 PET 영상 평가)

  • Yoon, Seok-Hwan
    • Journal of radiological science and technology
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    • v.41 no.4
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    • pp.321-327
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    • 2018
  • The purpose of this study is to compare PET imaging performance with Fluorine-18 ($^{18}F$) and Gallium-68 ($^{68}Ga$) for influence of physical properties of PET tracer. Measurement were performed on a Siemens Biograph mCT64 PET/CT scanner using NEMA IEC body phantom and Flangeless Esser PET phantom containing filled with $^{18}F$ and $^{68}Ga$. Emission scan duration(ESD) was set to 1, 2, 3, 4 and 5min/bed for $^{68}Ga$ and 1min/bed for $^{18}F$. The PET image were evaluated in terms of contrast, spatial resolution. Under same condition, The percentage of contrast recovery measured in the phantom ranged from 16.88% to 72.56% for $^{68}Ga$ and from 27.51% to 74.43% for $^{18}F$ and The FWHM value to evaluate spatial resolution was 10.96 mm for $^{68}Ga$ and 9.19 mm for $^{18}F$. For this study, $^{18}F$ produces better image contrast and spatial resolution than $^{68}Ga$ due to higher positron yield and lower positron energy ($^{18}F$: 96.86%, 633.5 keV, $^{68}Ga$: 88.9%, 1899 keV), The physical properties of PET tracer effect on the PET image. $^{68}Ga$ image applying ESD of 3, 4, 5min/bed were showed similar to $^{18}F$ image with ESD of 1min/bed. This study suggests that increasing ESD for acquiring $^{68}Ga$ PET image seem to be similar to $^{18}F$ image.

Material Properties and Shrinkage Crack Resistance of Concrete Produced with Fluorine-Silicate Hybrid Type Crack Reducing Agent (불소-실리카 복합형 균열저감제가 첨가된 콘크리트의 재료 특성과 수축균열 저항성)

  • Lee, Man-Ik;Park, Jong-Hwa;Nam, Jae-Hyun;Kim, Do-Su;Kim, Jae-On
    • Journal of the Korea Concrete Institute
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    • v.18 no.4 s.94
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    • pp.553-558
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    • 2006
  • In this study, fluorine-silicate hybrid type crack reducing agent(FS) consisted of fluorine and silicate compounds applied to concrete mix(specification : 25-30-18) between 0.5% and 2.0% at intervals of 0.5% based on cement weight. Experiments for material properties of concrete such as slump, air content and bleeding with elapsed time were performed. Experiment and elucidation for shrinkage crack resistance as well as adiabatic hydration temperature were also carried out. It was appeared that FS addition contributed to lower bleeding and hydration temperature without disturbance of fresh properties of concrete such as slump and air content compared to non-added concrete. Especially, shrinkage crack resistance of concrete resulted from plastic and drying shrinkage could be effectively reduced by the addition of FS ranging from 1.0% to 1.5%.