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1.
《Journal of labelled compounds & radiopharmaceuticals》2006,49(11):997-1006
Radiosynthesis of a novel substrate for histone deacetylase (HDAC), 6‐([18F]fluoroacetamido)‐1‐hexanoicanilide ([18F]FAHA, [18F]‐ 3 ) is reported. For precursor synthesis, compound 1 (6‐amino‐1‐hexanoicanilide) was prepared by the reaction of 6‐amino hexanoic acid with thionyl chloride in dichloroethane followed by addition of aniline. Compound 1 was reacted with bromoacetic anhydride in tetrahydrofuran (THF) in the presence of triethylamine to produce the precursor compound 6‐(bromoacetamido)‐1‐hexanoicanilide 2 . Fluorination reactions were performed using tetrabutylammonium fluoride in various solvents at 80°C to prepare the unlabeled reference compound 3 . Radiofluorinations were performed using either n‐Bu4N18F or K18F/kryptofix, and the crude product was purified by high performance liquid chromatography (HPLC). The radiochemical yields were 9–13% decay corrected (d.c.) with an average of 11% using K18F/kryptofix, and specific activity >2 GBq/µmol at the end of synthesis. The synthesis time was 67–75 min from the end of bombardment (EOB). Copyright © 2006 John Wiley & Sons, Ltd. 相似文献
2.
《Journal of labelled compounds & radiopharmaceuticals》2006,49(12):1079-1088
Syntheses of N‐3(substituted) analogues of thymidine, N‐3([18F]fluorobutyl)thymidine ([18F]‐FBT) and N‐3([18F]fluoropentyl)thymidine ([18F]‐FPT) are reported. 1,4‐Butane diol and 1,5 pentane diol were converted to their tosyl derivatives 2 and 3 followed by conversion to benzoate esters 4 and 5, respectively. Protected thymidine 1 was coupled separately with 4 and 5 to produce 6 and 7 , which were hydrolyzed to 8 and 9 , then converted to their mesylates 10 and 11 , respectively. Compounds 10 and 11 were fluorinated with n‐Bu4N[18F] to produce 12 and 13 , which by acid hydrolysis yielded 14 and 15 , respectively. The crude products were purified by HPLC to obtain [18F]‐FBT and [18F]‐FPT. The radiochemical yields were 58–65% decay corrected (d.c.) for 14 and 46–57% (d.c.) for 15 with an average of 56% in three runs per compound. Radiochemical purity was >99% and specific activity was >74 GBq/µmol at the end of synthesis (EOS). The synthesis time was 65–75 min from the end of bombardment (EOB). Copyright © 2006 John Wiley & Sons, Ltd. 相似文献
3.
L. Li L. Brichard L. Larsen D. K. Menon R. A. J. Smith M. P. Murphy F. I. Aigbirhio 《Journal of labelled compounds & radiopharmaceuticals》2013,56(14):717-721
Changes in the magnitude of the mitochondrial membrane potential occur in a range of important pathologies. To assess changes in membrane potential in patients, we set out to develop an improved mitochondria‐targeted positron emission tomography probe comprising a lipophilic triphenylphosphonium cation attached to a fluorine‐18 radionuclide via an 11‐carbon alkyl chain, which is well‐established to effectively transport to and localise within mitochondria. Here, we describe the radiosynthesis of this probe, 11‐[18F]fluoroundecyl‐triphenylphosphonium (MitoF), from no‐carrier‐added [18F]fluoride and a fully automated synthetic protocol to prepare it in good radiochemical yields (2–3 GBq at end‐of‐synthesis) and radiochemical purity (97–99%). Copyright © 2013 John Wiley & Sons, Ltd. 相似文献
4.
Vattoly J. Majo Norman R. Simpson Jaya Prabhakaran J. John Mann J. S. Dileep Kumar 《Journal of labelled compounds & radiopharmaceuticals》2014,57(13):705-709
Mammalian target of rapamycin (mTOR) plays a pivotal role in many aspects of cellular proliferation, and recent evidence suggests that an altered mTOR signaling pathway plays a central role in the pathogenesis of aging, tumor progression, neuropsychiatric, and major depressive disorder. Availability of a mTOR‐specific PET tracer will facilitate monitoring early response to treatment with mTOR inhibitors that are under clinical development. Towards this we have developed the radiosynthesis of [18F]1‐(4‐(4‐(8‐oxa‐3‐azabicyclo[3.2.1]octan‐3‐yl)‐1‐(2,2,2‐trifluoroethyl)‐1H‐pyrazolo[3,4‐d]pyrimidin‐6‐yl)phenyl)‐3‐(2‐fluoroethyl)urea [18F]ATPFU ([18F]1) as an mTOR PET ligand. Synthesis of reference 1 and the precursor for radiolabeling, 4‐(4‐8‐oxa‐3‐azabicyclo[3.2.1]‐octan‐3yl)‐1‐(2,2,2‐trifluoroethyl)‐1H‐pyrazolo[3,4‐d]pyrimidin‐6yl)aniline (10), were achieved from beta‐chloroaldehyde 3 in 4 and 5 steps, respectively, with an overall yield of 25–28%. [18F]Fluoroethylamine was prepared by heating N‐[2‐(toluene‐4‐sulfonyloxy)ethyl]phthalimide with [18F]fluoride ion in acetonitrile. [18F]1 was obtained by slow distillation under argon of [18F]FCH2CH2NH2 into amine 10 that was pre‐treated with triphosgene at 0–5 °C. The total time required for the two‐step radiosynthesis including semi‐preparative HPLC purification was 90 min, and the overall radiochemical yield of [18F]1 for the process was 15 ± 5% based on [18F]fluoride ion (decay corrected). At the end of synthesis (EOS), the specific activity was 37–74 GBq/µmol (N = 6). 相似文献
5.
《Journal of labelled compounds & radiopharmaceuticals》2004,47(8):469-476
3‐[18F]Fluoropropyl‐, 4‐[18F]fluorobenzyl‐triphenylphosphonium and 4‐[18F]fluorobenzyltris‐4‐dimethylaminophenylphosphonium cations were synthesized in multi‐step reactions from no carrier added (nca) [18F]fluoride. The time for synthesis, purification, and formulation was 56, 82, and 79 min with an average radiochemical yield of 12, 6 and 15%, respectively (not corrected for decay). The average specific radioactivity for the three radiolabeled compounds was 14.9 GB q/µmole (403 mCi/µmole) at end of synthesis (EOS). Copyright © 2004 John Wiley & Sons, Ltd. 相似文献
6.
Matthias Glaser Erik Årstad Sajinder K. Luthra Edward G. Robins 《Journal of labelled compounds & radiopharmaceuticals》2009,52(8):327-330
The acylation reagent [18F]N‐succinimidyl‐4‐fluorobenzoate (18F‐SFB) has been prepared using a new two‐step approach. The starting material p‐[18F]fluorobenzaldehyde (18F‐FBA) was obtained by an improved radiosynthesis with a decay‐corrected radiochemical yield of 66±6 % (n=3). Reaction of 18F‐FBA with (diacetoxyiodine)benzene and N‐hydroxysuccinimide and preparative HPLC purification furnished 18F‐SFB in an r.c.y. of 49±6 % (n=3), based on the starting radioactivity of 18F‐FBA. The radiochemical purity of 18F‐SFB was >99%. Alternatively, purification by solid phase extraction gave 18F‐SFB with an r.c.y. of 77±9% (n=4) and a radiochemical purity of 89±5% (n=4). This radiochemical synthesis only used non‐aqueous solvents, which simplifies the method and facilitates subsequent applications of 18F‐SFB. Copyright © 2009 John Wiley & Sons, Ltd. 相似文献
7.
Vincenzo Paolillo Stefan Riese Juri G. Gelovani Mian M. Alauddin 《Journal of labelled compounds & radiopharmaceuticals》2009,52(13):553-558
2′‐Deoxy‐2′‐[18F]fluoro‐5‐substituted‐1‐β‐D ‐arabinofuranosyluracils, including 2′‐deoxy‐2′‐[18F]fluoro‐5‐methyl‐1‐β‐D ‐arabinofuranosyluracil [18F]FMAU and [18F]FEAU are established radiolabeled probes to monitor cellular proliferation and herpes simplex virus type 1 thymidine kinase (HSV1‐tk) reporter gene expression with positron emission tomography. For clinical applications, a fully automated CGMP‐compliant radiosynthesis is necessary for production of these probes. However, due to multiple steps in the synthesis, no such automated synthetic protocols have been developed. We report here a fully automated synthesis of [18F]‐FEAU and [18F]‐FMAU on a prototype dual reactor module TRACERlab FX FN. The synthesis was performed by using a computer‐programmed standard operating procedure, and the product was purified on a semipreparative high‐performance liquid chromatography (HPLC) integrated with the synthesis module using 12% EtOH in 50 mM Na2HPO4. Finally, the percentage of alcohol was adjusted to 7% by adding Na2HPO4 and filtered through a Millipore filter to make dose for human. The radiochemical yield on the fluorination was 40±10% (n=10), and the overall yields were 4±1% (d. c.), from the end of the bombardment; [18F]FEAU (n=7) and [18F]FMAU (n=3). The radiochemical purity was >99%, specific activity was 1200–1300 mCi/µmol. The synthesis time was 2.5 h. This automated synthesis should be suitable for production of [18F]FIAU, [18F]FFAU, [18F]FCAU, [18F]FBAU and other 5‐substitued thymidine analogues. Copyright © 2009 John Wiley & Sons, Ltd. 相似文献
8.
《Journal of labelled compounds & radiopharmaceuticals》2005,48(8):547-555
The novel sigma‐1 receptor PET radiotracer [18F]1‐(2‐fluoroethyl)‐4‐[(4‐cyanophenoxy)methyl]piperidine ([18F]WLS1.002, [18F]‐2) was synthesized (n=6) by heating the corresponding N‐ethylmesylate precursor in an anhydrous acetonitrile solution containing [18F]fluoride, Kryptofix K222 and potassium carbonate for 15 min. Purification was accomplished by reverse‐phase HPLC methods, providing [18F]‐2 in 59±8% radiochemical yield (EOB), with specific activity of 2.89±0.80 Ci/µmol (EOS) and radiochemical purity of 98.3±2.1%. Rat biodistribution studies revealed relatively high uptake in many organs known to contain sigma‐1 receptors, including the lungs, kidney, heart, spleen, and brain. Good clearance from normal tissues was observed over time. Blocking studies (60 min) demonstrated high (>80%) specific binding of [18F]‐2 in the brain, with reduction also noted in other organs known to express these sites. Copyright © 2005 John Wiley & Sons, Ltd. 相似文献
9.
《Journal of labelled compounds & radiopharmaceuticals》2017,60(5):263-269
Fluorine‐18–labelled 6‐(fluoro)‐3‐(1H‐pyrrolo[2,3‐c]pyridin‐1‐yl)isoquinolin‐5‐amine ([18F]MK‐6240) is a novel potent and selective positron emission tomography (PET) radiopharmaceutical for detecting human neurofibrillary tangles, which are made up of aggregated tau protein. Herein, we report the fully automated 2‐step radiosynthesis of [18F]MK‐6240 using a commercially available radiosynthesis module, GE Healthcare TRACERlab FXFN. Nucleophilic fluorination of the 5‐diBoc‐6‐nitro precursor with potassium cryptand [18F]fluoride (K[18F]/K222) was performed by conventional heating, followed by acid deprotection and semipreparative high‐performance liquid chromatography under isocratic conditions. The isolated product was diluted with formulation solution and sterile filtered under Current Good Manufacturing Practices, and quality control procedures were established to validate this radiopharmaceutical for human use. At the end of synthesis, 6.3 to 9.3 GBq (170‐250 mCi) of [18F]MK‐6240 was formulated and ready for injection, in an uncorrected radiochemical yield of 7.5% ± 1.9% (relative to starting [18F]fluoride) with a specific activity of 222 ± 67 GBq/μmol (6.0 ± 1.8 Ci/μmol) at the end of synthesis (90 minutes; n = 3). [18F]MK‐6240 was successfully validated for human PET studies meeting all Food and Drug Administration and United States Pharmacopeia requirements for a PET radiopharmaceutical. The present method can be easily adopted for use with other radiofluorination modules for widespread clinical research use. 相似文献
10.
Ofer Shamni Bruno Nebeling Hilbert Grievink Eyal Mishani 《Journal of labelled compounds & radiopharmaceuticals》2019,62(6):252-258
Radiolabeled prostate‐specific membrane antigen (PSMA) targeting PET‐tracers have become desirable radiopharmaceuticals for the imaging of prostate cancer (PC). Recently, the PET radiotracer [18F]PSMA‐1007 was introduced as an alternative to [68Ga]Ga‐PSMA‐11, for staging and diagnosing biochemically recurrent PC. We incorporated a one‐step procedure for [18F]PSMA‐1007 radiosynthesis, using both Synthra RNplus and GE TRACERlab FxFN automated modules, in accordance with the recently described radiolabeling procedure. Although the adapted [18F]PSMA‐1007 synthesis resulted in repeatable radiochemical yields (55 ± 5%, NDC), suboptimal radiochemical purities of 87 ± 8% were obtained using both modules. As described here, modifications made to the radiolabeling and the solid‐phase extraction purification steps reduced synthesis time to 32 minutes and improved radiochemical purity to 96.10%, using both modules, without shearing the radiochemical yield. 相似文献
11.
An improved synthesis of the radiolabeled prostate‐specific membrane antigen inhibitor, [18F]DCFPyL
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Hayden T. Ravert Daniel P. Holt Ying Chen Ronnie C. Mease Hong Fan Martin G. Pomper Robert F. Dannals 《Journal of labelled compounds & radiopharmaceuticals》2016,59(11):439-450
The radiosynthesis of [18F]DCFPyL on 2 distinct automated platforms with full regulatory compliant quality control specifications is described. The radiotracer synthesis was performed on a custom‐made radiofluorination module and the Sofie Biosciences ELIXYS. The radiofluorination module synthesis was accomplished in an average of 66 minutes from end of bombardment with an average specific activity at end of synthesis (EOS) of 4.4 TBq/μmol (120 Ci/μmol) and an average radiochemical yield of 30.9% at EOS. The ELIXYS synthesis was completed in an average of 87 minutes with an average specific activity of 2.2 TBq/μmol (59.3 Ci/μmol) and an average radiochemical yield of 19% at EOS. Both synthesis modules produced large millicurie quantities of [18F]DCFPyL while conforming to all standard US Pharmacopeia Chapter <823> acceptance testing criteria. 相似文献
12.
Scott M. Apana Robert J. Griffin Nathan A. Koonce Jessica S. Webber Ruud P. M. Dings Kevin H. Mayo Marc S. Berridge 《Journal of labelled compounds & radiopharmaceuticals》2011,54(11):708-713
Anginex is a 33‐residue peptide that has been previously demonstrated to possess antiangiogenic properties. To provide a tool to evaluate the regional biodistribution and pharmacokinetics of anginex, and possibly to provide a useful angiogenesis‐targeted radiotracer, we have radiolabeled anginex with fluorine‐18. High specific activity [18F]fluorobenzaldehyde (1.5–4.8 TBq (40–130 Ci)/µmol) was used to label anginex via reductive amination in 76% yield. The effective specific activity of the product was lower because unlabeled anginex was not separated. However, the high specific activity labeling reagent increased the labeling yield and reduced the amount of anginex required for labeling. Regional pharmacokinetics were measured by PET scanning in mice, demonstrating tumor uptake and low background, with up to 30% of total injected dose localized in some tumors. Copyright © 2011 John Wiley & Sons, Ltd. 相似文献
13.
Annelaure Damont Françoise Hinnen Bertrand Kuhnast Marie‐Anne Schöllhorn‐Peyronneau Michelle James Christopher Luus Bertrand Tavitian Michael Kassiou Frédéric Dollé 《Journal of labelled compounds & radiopharmaceuticals》2008,51(7):286-292
Recently, a novel series of 2‐phenylpyrazolo[1,5‐a]pyrimidineacetamides has been reported as selective ligands of the translocator protein (18 kDa). Within this series, DPA‐714 (N,N‐diethyl‐2‐(2‐(4‐(2‐fluoroethoxy)phenyl)‐5,7‐dimethylpyrazolo[1,5‐a]pyrimidin‐3‐yl)acetamide, Ki=7.0 nM) is a compound, which had been designed with a fluorine atom in its structure, allowing labelling with fluorine‐18 (half‐life: 109.8 min) and in vivo imaging using positron emission tomography. DPA‐714 and its tosyloxy derivative (N,N‐diethyl‐2‐(2‐(4‐(2‐toluenesulfonyloxyethoxy)phenyl)‐5,7‐dimethylpyrazolo[1,5‐a]pyrimidin‐3‐yl)acetamide) as precursor for the labelling with fluorine‐18 were synthesized in two steps from DPA‐713 (N,N‐diethyl‐2‐(2‐(4‐methoxyphenyl)‐5,7‐dimethylpyrazolo[1,5‐a]pyrimidin‐3‐yl)acetamide) and obtained in 32 and 42% yields, respectively. [18F]DPA‐714 was synthesized using a simple one‐step process (a tosyloxy‐for‐fluorine nucleophilic aliphatic substitution), which has been fully automated on our Zymate‐XP robotic system. It involves: (A) reaction of K[18F]F‐Kryptofix®222 with the tosyloxy precursor (4.5–5.0 mg, 8.2–9.1 µmol) at 165°C for 5 min in dimethyl sufloxide (0.6 mL) followed by (B) C18 PrepSep cartridge pre‐purification and finally (C) semi‐preparative high‐performance liquid chromatography (HPLC) purification on a Waters X‐Terra? RP18. Typically, 5.6–7.4 GBq of [18F]DPA‐714 (>95% chemically and radiochemically pure) could be obtained with specific radioactivities ranging from 37 to 111 GBq/µmol within 85–90 min (HPLC purification and SepPak®‐based formulation included), starting from a 37 GBq [18F]fluoride batch (overall non‐decay‐corrected and isolated radiochemical yield: 15–20%). Copyright © 2008 John Wiley & Sons, Ltd. 相似文献
14.
《Journal of labelled compounds & radiopharmaceuticals》2005,48(13):941-950
The synthesis of a pyrimidine analog, 3′‐deoxy‐3′‐[18F]‐fluoro‐1‐β‐D ‐xylofuranosyluracil ([18F]‐FMXU) is reported. 5‐Methyluridine 1 was converted to its di‐methoxytrityl derivatives 2 and 3 as a mixture. After separation the 2′,5′‐di‐methoxytrityluridine 2 was converted to its 3′‐triflate 4 followed by derivatization to the respective N3‐t‐Boc product 5 . The triflate 5 was reacted with tetrabutylammonium[18F]fluoride to produce 6 , which by acid hydrolysis yielded compound 7 . The crude preparation was purified by HPLC to obtain the desired product [18F]‐FMXU. The radiochemical yields were 25–40% decay corrected (d. c.) with an average of 33% in four runs. Radiochemical purity was >99% and specific activity was >74 GBq/µmol at the end of synthesis (EOS). The synthesis time was 67–75 min from the end of bombardment (EOB). Copyright © 2005 John Wiley & Sons, Ltd. 相似文献
15.
Matthias Glaser Erik Årstad Alessandra Gaeta James Nairne William Trigg Edward G. Robins 《Journal of labelled compounds & radiopharmaceuticals》2012,55(9):326-331
18F‐labelled fluoroalkylamines are attractive reagents for the preparation of positron emission tomography tracers containing amine, amide, and N‐heterocyclic moieties. Herein, we report that 2‐[18F]fluoroethylamine can be obtained from 2‐[18F]fluoroethyl azide by reduction with elemental copper under acidic conditions. Azide to amine reduction was achieved in near quantitative analytical yields within 30 min by heating a solution of 2‐[18F]fluoroethyl azide in the presence of copper wire and aqueous trifluoroacetic acid. Subsequent reaction of 2‐[18F]fluoroethylamine with benzoyl chloride in the presence of triethylamine provided N‐[18F]fluoroethyl benzamide in 63% decay‐corrected radiochemical yield from 2‐[18F]fluoroethyl azide. The utility of the Cu(0)/H+ azide reduction method was further exemplified by preparation of the potential GABAA tracer 9H‐β‐carboline N‐2‐[18F]fluoroethylamide, which was obtained in 46% decay‐corrected radiochemical yield by reaction of 2‐[18F]fluoroethylamine with the corresponding 9H‐β‐carboline pentafluorophenyl ester. Copyright © 2012 John Wiley & Sons, Ltd. 相似文献
16.
William P. Tong Juri G. Gelovani Mian M. Alauddin 《Journal of labelled compounds & radiopharmaceuticals》2011,54(5):233-238
Introduction: The hepatocellular carcinoma–intestine–pancreas and pancreatitis‐associated proteins, also known as lactose‐binding protein, is upregulated in peritumoral pancreatic tissue. Previously, we reported ethyl‐ β ‐D ‐galactopyranosyl‐(1,4′)‐2′‐deoxy‐2′‐[18F]fluoro‐ β ‐D ‐glucopyranoside (Et‐[18F]‐FDL), a radiofluorinated lactose analog for positron emission tomography (PET) of small pancreatic carcinomas in mice. However, synthesis of the precursor for Et‐[18F]‐FDL involves 11 steps, which is quite lengthy, and produces overall low yields. Here, we report on synthesis and radiolabeling of another analog of lactose, the 1′‐[18F]fluoroethyl‐ β ‐D ‐lactose for PET imaging of pancreatic carcinomas. Methods: Two precursor compounds, 1′‐bromoethyl‐2′,3′,6′,2,3,4,6‐hepta‐O‐acetyl‐ β ‐D ‐lactose 4, and 1′‐p‐toluenesulfonylethyl‐2′,3′,6′,2,3,4,6‐hepta‐O‐acetyl‐ β ‐D ‐lactose 5, were synthesized in two and three steps, respectively; then, cold fluorination and radiofluorination of these precursors were performed. The reaction mixture was passed through a silica gel Sep‐pack cartridge, eluted with EtOAc, and the 1′‐[18F]fluoroethyl‐2′,3′,6′,2,3,4,6‐hepta‐O‐acetyl‐ β ‐D ‐lactose ([18F]‐6) purified by HPLC. After hydrolysis of the protecting groups, the 1′‐[18F]fluoroethyl‐ β ‐D ‐lactose [18F]‐7 was neutralized, diluted with saline, filtered through a sterile Millipore filter, and analyzed by radio‐TLC. Results: The average decay‐corrected radiochemical yield was 9% (n = 7) with>99% radiochemical purity and specific activity of 55.5 GBq/ µ mol. Conclusion : A new analog of lactose, 1′‐[18F]fluoroethyl‐ β ‐D ‐lactose, has been synthesized in good yields, with high purity and high specific activity suitable for PET imaging of early pancreatic carcinomas. Copyright © 2011 John Wiley & Sons, Ltd. 相似文献
17.
《Journal of labelled compounds & radiopharmaceuticals》2003,46(9):805-814
The syntheses of adenosine analogues, 2′‐deoxy‐2′‐[18F]fluoro‐9‐β‐D ‐arabinofuranosyladenine ([18F]‐FAA) and 3′‐deoxy‐3′‐[18F]fluoro‐9‐β‐D ‐xylofuranosyladenine ([18F]‐FXA) are reported. Adenosine ( 1 ) was converted to its methoxytrityl derivatives 2 and 3 as a mixture. After separation, these derivatives were converted to their respective triflates 4 and 5 . Each triflate was reacted with tetrabutylammonium[18F]fluoride to produce 6b or 7b , which by acidic hydrolysis yielded compounds 8b and 9b . Crude preparations were purified by HPLC to obtain the desired pure products. The radiochemical yields were 10‐18% decay corrected (d. c.) for 8b and 30‐40% (d. c.) for 9b in 4 and 3 runs, respectively. Radiochemical purity was >99% and specific activity was >74 GBq/μmol at the end of synthesis (EOS). The synthesis time was 90‐95 min from the end of bombardment (EOB). Copyright © 2003 John Wiley & Sons, Ltd. 相似文献
18.
Pradip Ghosh Juri G. Gelovani Mian M. Alauddin 《Journal of labelled compounds & radiopharmaceuticals》2007,50(13):1185-1191
Radiosyntheses of two N3‐substituted thymidine analogues, N3‐[(4[18F]fluoromethyl‐phenyl)butyl]thymidine ([18F]‐FMPBT) and N3‐[(4[18F]fluoromethyl‐phenyl)pentyl]thymidine ([18F]‐FMPPT), are reported. The precursor compounds 9 and 10 were synthesized in six steps and the standard compounds 13 and 14 were synthesized from these precursors. For radiosynthesis, compounds 9 and 10 were fluorinated with n‐Bu4N[18F] to produce [18F]‐ 11 and [18F]‐ 12 , which by acid hydrolysis yielded [18F]‐ 13 and [18F]‐ 14 , respectively. The crude products were purified by high‐performance liquid chromatography to obtain [18F]‐FMPBT and [18F]‐FMPPT. The average decay‐corrected radiochemical yield for [18F]‐ 13 was 15% in five runs, and that for [18F]‐ 14 was 10% in four runs. The radiochemical purity was >99% and the specific activity was >74 GBq/µmol at the end of synthesis. The synthesis time was 80–90 min from the end of bombardment. Copyright © 2007 John Wiley & Sons, Ltd. 相似文献
19.
Salla Lahdenpohja Thomas Keller Johan Rajander Anna K. Kirjavainen 《Journal of labelled compounds & radiopharmaceuticals》2019,62(6):259-264
[18F]NS12137 (exo‐3‐[(6‐[18F]fluoro‐2‐pyridyl)oxy]8‐azabicyclo[3.2.1]octane) is a highly selective norepinephrine transporter (NET) tracer. NETs are responsible for the reuptake of norepinephrine and dopamine and are linked to several neurodegenerative and neuropsychiatric disorders. The aim of this study was to develop a copper‐mediated 18F‐fluorination method for the production of [18F]NS12137 with straightforward synthesis conditions and high radiochemical yield and molar activity. [18F]NS12137 was produced in two steps. Radiofluorination of [18F]NS12137 was performed via a copper‐mediated pathway starting with a stannane precursor and using [18F]F? as the source of the fluorine‐18 isotope. Deprotection was performed via acid hydrolysis. The radiofluorination reaction was nearly quantitative as was the deprotection based on HPLC analysis. The radiochemical yield of the synthesis was 15.1 ± 0.5%. Molar activity of [18F]NS12137 was up to 300 GBq/μmol. The synthesis procedure is straightforward and can easily be automated and adapted for clinical production. 相似文献
20.
《Journal of labelled compounds & radiopharmaceuticals》2005,48(2):109-115
Acrylamido‐quinazolines substituted at the 6‐position bind irreversibly to the intracellular ATP binding domain of the epidermal growth factor receptor (EGFR). A general route was developed for preparing 6‐substituted‐4‐anilinoquinazolines from [18F]fluoroanilines for evaluation as EGFR targeting agents with PET. By a cyclization reaction, 2‐[18F]fluoroaniline was reacted with N′‐(2‐cyano‐4‐nitrophenyl)‐N,N‐dimethylimidoformamide to produce 6‐nitro‐4‐(2‐[18F]fluoroanilino)quinazoline in 27.5% decay‐corrected radiochemical yield. Acid mediated tin chloride reduction of the nitro group was achieved in 5 min (80% conversion) and subsequent acylation with acrylic acid gave 6‐acrylamido‐4‐(2‐[18F]fluoroanilino)quinazoline in 8.5% decay‐corrected radiochemical yield, from starting fluoride, in less than 2 h. Copyright © 2005 John Wiley & Sons, Ltd. 相似文献