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Facile synthesis of 2‐deoxy‐2‐[18F]fluorosorbitol using sodium borohydride on aluminum oxide J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-10-16 Koki Hasegawa; Kazuhiro Koshino; Takahiro Higuchi
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Use of radioiodine in nuclear medicine a ‐ brief overview J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-10-22 Trevor Ferris; Laurence Carroll; Sarah Jenner; Eric O. Aboagye
Radioiodines have a long history in nuclear medicine. Herein we discuss the production, properties and applications of these versatile iodine‐based imaging and theragnostic agents. There are 38 isotopes of iodine (I) including one stable form (127I). The most common radionuclides used in medical imaging and treatment, including Iodine‐123 (123I), Iodine‐124 (124I), Iodine‐125 (125I) and Iodine‐131
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Development of a novel [18F]fluorobenzyl derivative of the AT1 Receptor antagonist Candesartan J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-10-20 Luis Michel Alonso Martinez; Jean N. DaSilva
Candesartan is a clinically‐approved angiotensin II type 1 receptor (AT1R)‐blocker that selectively binds AT1Rs in high affinity. We report here the radiosynthesis and automation of the novel [18F]fluorobenzyl derivative of Candesartan using the Sonogashira cross‐coupling reaction. [18F]Fluorobenzyl‐Candesartan was developed from 4‐[18F]fluoroiodobenzene ([18F]FIB) that was conjugated with alkyne‐trityl‐candesartan
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Automated radiosynthesis of [68Ga]Ga‐PSMA‐11 and [177Lu]Lu‐PSMA‐617 on the iPHASE MultiSyn module for clinical applications J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-10-17 Christian W. Wichmann; Uwe Ackermann; Stan Poniger; Kenneth Young; Benjamin Nguyen; Gordon Chan; John Sachinidis; Andrew M. Scott
PSMA‐targeted imaging and therapy of prostate cancer using theranostic pairs is rapidly changing clinical practice. To facilitate clinical trials, fully automated procedures for the radiosyntheses of [68Ga]Ga‐PSMA‐11 and [177Lu]Lu‐PSMA‐617 were developed from commercially available precursors using the cassette based iPHASE MultiSyn module. Formulated and sterile radiopharmaceuticals were obtained
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Radiosynthesis and quality control testing of the tau imaging PET tracer [18F]PM‐PBB3 for clinical applications J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-10-17 Kazunori Kawamura; Hiroki Hashimoto; Kenji Furutsuka; Takayuki Ohkubo; Tomoya Fujishiro; Takahiro Togashi; Daisuke Arashi; Toshiyuki Sakai; Masatoshi Muto; Masanao Ogawa; Yusuke Kurihara; Nobuki Nengaki; Makoto Takei; Kazuyoshi Nemoto; Makoto Higuchi; Ming‐Rong Zhang
Recently, we produced 11C‐labeled 2‐((1E,3E)‐4‐(6‐(methylamino)pyridin‐3‐yl)buta‐1,3‐dienyl)benzo[d]thiazol‐6‐ol ([11C]PBB3) as a clinically useful positron emission tomography (PET) tracer for in vivo imaging of tau pathologies in the human brain. To overcome the limitations (i.e., rapid in vivo metabolism and short half‐life) of [11C]PBB3, we further synthesized 18F‐labeled 1‐fluoro‐3‐((2‐((1E,3
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Production of the next‐generation positron nuclide zirconium‐89 (89Zr) guided by Monte Carlo simulation and its good quality for antibody labeling J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-10-17 Feng Wang; Jin Ding; Xiaoyi Guo; Teli Liu; Lixin Ding; Lei Xia; Hua Zhu; Zhi Yang
The next‐generation positron zirconium‐89(89Zr, T1/2 = 3.27 days) is a novel nuclide for immuno‐PET because of its favorite longer half‐life. The aim of this work is to develop optimized methods for routine production and purification of 89Zr through Monte Carlo (MC) simulation and laboratory experiments. 89Y(p,n)89Zr reaction was used for 89Zr production. Optimized thicknesses of Al degrader (0.11
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A highly reproducible method for the measurement of [6‐O‐methyl‐11C]diprenorphine and its radio‐metabolites based on solid phase extraction (SPE) and radio‐HPLC J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-10-16 Michael Fairclough; Adam McMahon; Elizabeth Barnett; Julian Matthews; Christopher A. Brown; Anthony Jones
Described here is a method for the measurement of the radio‐metabolites of the positron emission tomography (PET) radiotracer [6‐O‐methyl‐11C]diprenorphine ([11C]diprenorphine) using in‐line solid phase extraction (SPE) combined with radio‐HPLC analysis. We believe that this method offers a reliable and reproducible approach to [11C]diprenorphine metabolite analysis. In addition, different SPE stationary
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Synthesis of 13C‐labelled cutin and suberin monomeric dicarboxylic acids of the general formula HO213C‐(CH2)n‐13CO2H (n = 10, 12, 14, 16, 18, 20, 22, 24, 26, 28) J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-10-16 Carina Schink; Sandra Spielvogel; Wolfgang Imhof
13C‐labelled dicarboxylic acids HO213C‐(CH2)n‐13CO2H (n = 10, 12, 14, 16, 18, 20, 22, 24, 26, 28) have been synthesized as internal standards for LC‐MS and GC‐MS analysis of cutin and suberin monomer degradation by soil based microorganisms. Different synthetic strategies had to be applied depending on the chain length of the respective synthetic target and due to economic considerations. 13C‐labels
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Dual‐labeled prostate‐specific membrane antigen (PSMA)‐targeting agent for preoperative molecular imaging and fluorescence‐guided surgery for prostate cancer J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-10-10 Myoung Hyoun Kim; Seul‐Gi Kim; Dae‐Weung Kim
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Synthesis of 18 F-radiolabeled organophosphine fluorides for thiol-chemoselective peptide conjugation. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-09-19 Huanglan Zhuang,Zhide Guo,Rongqiang Zhuang,Xianzhong Zhang
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Radiolabeled hormones in insulin research, a minireview. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-09-09 J Jiráček,L Žáková,A Marek
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Issue Information J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-10-05
No abstract is available for this article.
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Thorium chelators for targeted alpha therapy: Rapid chelation of thorium-226. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-08-18 Maryline G Ferrier,Yawen Li,Ming-Kuan Chyan,Roger Wong,Lily Li,Sarah Spreckelmeyer,Donald K Hamlin,Tara Mastren,Michael E Fassbender,Chris Orvig,D Scott Wilbur
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Study the 99mTc‐labeling conditions of HYNIC‐conjugated peptides from a new perspective: Introduction to the term radio‐stoichiometry J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-09-30 Sajad Kaihani; Nourollah Sadeghzadeh
Specific tumor uptake of peptide radiopharmaceuticals depends on tumor binding affinity and their radiochemical purity. Several important parameters that influence the 99mTc‐labeling and consequently the radiochemical purity of HYNIC‐conjugated peptide are radionuclide activity, the amount of peptide, the amount of co‐ligands, and the amount of reducing agents (stannous ion). In this review article
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Synthesis of a Deuterated 6-AmHap Internal Standard for the Determination of Hapten Density in a Heroin Vaccine Drug Product. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-09-02 Mariia Makarova,Rodell C Barrientos,Oscar B Torres,Gary R Matyas,Arthur E Jacobson,Agnieszka Sulima,Kenner C Rice
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Studies of hydrogen isotope scrambling during the dehalogenation of aromatic chloro-compounds with deuterium gas over palladium catalysts. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-09-04 William J S Lockley,Niccolò A E Venanzi,Georgie J Crane
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Issue Information J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-09-13
No abstract is available for this article.
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Enantioselective synthesis of tri-deuterated (-)-geosmin to be used as internal standard in quantitation assays. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-07-28 Caterina Porcelli,Johanna Kreissl,Martin Steinhaus
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Radiosynthesis of a Bruton's tyrosine kinase inhibitor, [11 C]Tolebrutinib, via palladium-NiXantphos-mediated carbonylation. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-07-29 Kenneth Dahl,Timothy Turner,Neil Vasdev
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Production of [68 Ga]Ga-PSMA: Comparing a manual kit-based method with a module-based automated synthesis approach. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-08-31 Janke Kleynhans,Sietske Rubow,Jannie le Roux,Biljana Marjanovic-Painter,Jan Rijn Zeevaart,Thomas Ebenhan
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Synthesis of stable-isotope-labeled N-(3-dimethylaminopropyl)-N'-ethylcarbodiimide and N-(3-dimethylaminopropyl)-N'-ethylurea. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-08-26 Kai Cao,John A Brailsford,Samuel J Bonacorsi
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Carbon-13 synthesis and NMR spectroscopic geometric isomer evaluation to support the filing of teriflunomide. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-08-24 Michael Kurz,Dirk Gretzke,Rolf Hörlein,Sandrine Turpault,Jens Atzrodt,Volker Derdau
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Issue Information J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-08-12
No abstract is available for this article.
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Iodination of CART(61-102) peptide: Preserved binding and anorexigenic activity in mice. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-07-17 Veronika Pražienková,Aleš Marek,Lenka Maletínská
CART (cocaine‐ and amphetamine‐regulated transcript) peptides are involved in food intake regulation, stress, and other physiological functions. Although CART peptides have been known for over 25 years, their receptor(s) have not yet been characterized. In this short review, we will summarize our previous studies, where we reported specific binding of 125I‐CART(61‐102) to PC12 rat pheochromocytoma
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Radiolabeled HOCPCA as a highly useful tool in drug discovery and pharmacology J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-07-20 Nane Griem‐Krey; Bente Frølund; Aleš Marek; Petrine Wellendorph
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Issue Information J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-07-23
No abstract is available for this article.
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S-(4-nitrobenzyl)-6-thioinosine: Tritium labelling at high specific activity. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-07-23 Crist N Filer,Chang Byon
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The magic of small structure differences in a sodium-glucose cotransporter drug discovery project-14 C-labelled drug candidates in a key-differentiating study. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-07-07 Manfred Schudok,Heiner Glombik,Volker Derdau
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The synthesis of one H-2 labeled and two H-3 labeled leukotriene C4 synthase inhibitors. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-07-07 Jonas Bergare,Lee Kingston,Dominic J Guly,James Dolan,Richard J Lewis,Charles S Elmore
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Radiosynthesis, in vitro and preliminary biological evaluation of [18 F]2-amino-4-((2-((3-fluorobenzyl)oxy)benzyl)(2-((3-(fluoromethyl)benzyl)oxy)benzyl)amino)butanoic acid, a novel alanine serine cysteine transporter 2 inhibitor-based positron emission tomography tracer. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-07-06 Tristan Baguet,Jakob Bouton,Jonas Janssens,Glenn Pauwelyn,Jeroen Verhoeven,Benedicte Descamps,Serge Van Calenbergh,Christian Vanhove,Filip De Vos
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Synthesis of C-14 labeled Rac-(3R,2S)-glycopyrronium bromide. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-07-01 Jonas Bergare,Neil Nixon,Jeffery Newsome,Linda Thunberg,Charles S Elmore
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Automated GMP production and long-term experience in radiosynthesis of CB1 tracer [18 F]FMPEP-d2. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-07-01 Salla Lahdenpohja,Thomas Keller,Sarita Forsback,Tapio Viljanen,Esa Kokkomäki,Riikka V Kivelä,Jörgen Bergman,Olof Solin,Anna K Kirjavainen
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New synthesis of 6″-[18 F]fluoromaltotriose for positron emission tomography imaging of bacterial infection. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-06-29 Moustafa T Gabr,Tom Haywood,Gayatri Gowrishankar,Ananth Srinivasan,Sanjiv S Gambhir
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Development of a fully automated low-pressure [11 C]CO carbonylation apparatus. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-06-25 Mélodie Ferrat,Youssef El Khoury,Peter Larsen,Kenneth Dahl,Christer Halldin,Magnus Schou
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PET Imaging of a Novel Anxal-targeted Peptide 18 F-Al-NODA-Bn-p-SCN-GGGRDN-IF7 in A431 Cancer Mouse Models. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-06-20 Fei Chen,Yichun Xiao,Kejing Shao,Bao Zhu,Mengjun Jiang
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Issue Information J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-06-18
No abstract is available for this article.
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A one-pot radiosynthesis of [18 F]PARPi. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-06-16 Thomas C Wilson,Nagavarakishore Pillarsetty,Thomas Reiner
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Issue Information J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-06-05
No abstract is available for this article.
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Automated synthesis of 68 Ga/177 Lu-PSMA on the Trasis miniAllinOne. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-06-01 Mikkel A Sørensen,Valdemar L Andersen,Helle Westergren Hendel,Charles Vriamont,Corentin Warnier,Julien Masset,Tri Hien Viet Huynh
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A novel 99m Tc-diester complex as tumor targeting agent: Synthesis, radiolabeling, and biological distribution study. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-05-19 Hesham A Shamsel-Din,Mohamed A Gizawy,Elsayed G Zaki,Amr Elgendy
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Issue Information J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-05-17
No abstract is available for this article.
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Synthesis of stable isotope-labelled firocoxib. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-05-05 Bachir Latli,Amy Gao,Valerie Kvaternick,Berhane Tecle,Scott Pennino,Nathan K Yee,Jeff Song
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Issue Information J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-05-04
No abstract is available for this article.
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Selective synthesis of L-2-[18 F]fluoro-alpha-methylphenylalanine via copper-mediated 18 F-fluorination of (mesityl)(aryl)iodonium salt. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-04-28 Aiko Yamaguchi,Hirofumi Hanaoka,Tetsuya Higuchi,Yoshito Tsushima
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Issue Information J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-04-05
No abstract is available for this article.
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Radiosynthesis of novel N-18 F-labeled 18 F-FHex-α-l-Glu and 18 F-FHex-β-Glu. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-03-30 Fuhua Wen,Shaoyu Liu,Hui Ma,Ganghua Tang
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Arabinofuranose-derived positron-emission tomography radiotracers for detection of pathogenic microorganisms. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-03-28 Mausam Kalita,Matthew F L Parker,Justin M Luu,Megan N Stewart,Joseph E Blecha,Henry F VanBrocklin,Michael J Evans,Robert R Flavell,Oren S Rosenberg,Michael A Ohliger,David M Wilson
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Nanoparticulate formulations of radiopharmaceuticals: Strategy to improve targeting and biodistribution properties J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-03-27 Pallab Datta, Soumendranath Ray
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Synthesis of isotopically labelled αCGRP8‐37 and its lipidated analogue J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-03-25 Benjamin L. Lu, Kerry M. Loomes, Debbie L. Hay, Paul W.R. Harris, Margaret A. Brimble
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Radiolabeled (R)-(-)-5-iodo-3'-O-[2-(ε-guanidinohexanoyl)-2-phenylacetyl]-2'-deoxyuridine: A new theranostic for neuroblastoma. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-03-19 Zbigniew P Kortylewicz,Don W Coulter,Guang Han,Janina Baranowska-Kortylewicz
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Cover Image J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-03-17 Lu Wang, Shaobo Yao, Ruikun Tang, Honghao Zhu, Lingling Zhang, Jian Gong, Qiusong Chen, Thomas Lee Collier, Hao Xu, Steven H. Liang
The cover image is based on the Research Article A concisely automated synthesis of TSPO radiotracer [18F]FDPA based on spirocyclic iodonium ylide method and validation for human use by Lu Wang et al., https://doi.org/10.1002/jlcr.3824.
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Issue Information J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-03-17
No abstract is available for this article.
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A 64 Cu-porphyrin-based dual-modal molecular probe with integrin αv β3 targeting function for tumour imaging. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-03-06 Di Fan,Kai Wang,Hannan Gao,Qi Luo,Xin Wang,Xiaotong Li,Wu Tong,Xin Zhang,Chuangwei Luo,Guangjie Yang,Lin Ai,Jiyun Shi
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Development of an automated, GMP compliant FASTlabTM radiosynthesis of [18 F]GE-179 for the clinical study of activated NMDA receptors. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-03-05 Imtiaz Khan,Tom Christian Berg,Jane Brown,Rajiv Bhalla,Anthony Wilson,Andrew Black,Graeme McRobbie,James Nairne,Andreas Olsson,William Trigg
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Manual vs automated 68Ga‐radiolabelling—A comparison of optimized processes J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-02-26 Michael Meisenheimer; Stefan Kürpig; Markus Essler; Elisabeth Eppard
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An alternative and simple synthesis of [14 C]potassium cyanate. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-02-13 Crist N Filer,C T Peng
The one‐step synthesis of [14C]potassium cyanate from [14C]urea is described with product characterization by gravimetric specific activity as well as a novel TLC system. The storage, stability, and repurification of [14C]potassium cyanate are also discussed.
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Synthesis of [3 H] and [14 C]genipin. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-02-11 Adele E Queen,David Hesk,David M Lindsay,William J Kerr,Kenneth Rehder,Tim Fennell,Wayne Mascarella,Desong Zhong,Scott Runyon
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Recent advances in iridium(I) catalysis towards directed hydrogen isotope exchange. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-02-11 William J Kerr,Gary J Knox,Laura C Paterson
The initial discovery and establishment of a family of novel iridium catalysts possessing N‐heterocyclic carbene units alongside bulky phosphine ligands allowed selected substrates to be labelled using deuterium or tritium gas at desirably low catalyst loadings via an ortho‐directed C―H insertion process. Such a method has broad applicability and offers distinct advantages within the pharmaceutical
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Automated radiosynthesis of [11 C]UCB-J for imaging synaptic density by positron emission tomography. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-02-06 Selena Milicevic Sephton,Tunde Miklovicz,Joseph J Russell,Aniruddha Doke,Lei Li,Istvan Boros,Franklin I Aigbirhio
An automated radiosynthesis of carbon‐11 positron emission tomography radiotracer [11C]UCB‐J for imaging the synaptic density biomarker synaptic vesicle glycoprotein SV2A was established using Synthra RNPlus synthesizer. Commercially available trifluoroborate UCB‐J analogue was used as a radiolabelling precursor, and the desired radiolabelled product was isolated in 11 ± 2% (n = 7) nondecay corrected
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Synthesis of imatinib, a tyrosine kinase inhibitor, labeled with carbon-14. J. Label. Comp. Radiopharm. (IF 1.809) Pub Date : 2020-02-05 Julie Kang,Jun Young Lee,Jeong-Hoon Park,Dong-Jo Chang
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