The synthesis of one H ‐2 labeled and two H‐3 labeled leukotriene C4 synthase inhibitors
As part of a medicinal chemistry program aimed at developing a leukotriene C4 synthase inhibitor for the treatment of asthma, two tritium labeled and one stable isotope labeled compounds were required. The synthesis of the tritium labeled compounds used a standard bromination ‐tritiodehalogentation approach. One of the tritium labeled compounds was observed to exchange its tritium label slowly with the solvent. The stable isotope labeled compound was prepared in seven steps (3% overall yield) from [2H6]acetone in a modification of the route used by medicinal chemistry. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - May 22, 2020 Category: Biochemistry Authors: Jonas Bergare, Lee Kingston, Dominic J. Guly, James Dolan, Richard J. Lewis, Charles S. Elmore Tags: RESEARCH ARTICLE Source Type: research

A novel 99mTc ‐diester complex as tumor targeting agent: Synthesis, radiolabeling, and biological distribution study
A novel diester (10 ‐[2‐(9‐carboxynonanoyloxy)propoxy]‐10‐oxodecanoic acid) was successfully synthesized in a good yield and radiolabeled with 99mTc in a high radiochemical yield. The new synthesized diester was characterized by different spectral techniques and its anticancer activity was also evaluated agai nst breast cancer cell line. The preclinical biodistribution study in tumor bearing mice revealed that 99mTc‐diester has high T/NT ratio and accumulated selectively in tumor cells, so it can be used as a promising candidate for solid tumor imaging. The target of this study is the synthesis of a new diester...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - May 19, 2020 Category: Biochemistry Authors: Hesham A. Shamsel ‐Din, Mohamed A. Gizawy, Elsayed G. Zaki, Amr Elgendy Tags: RESEARCH ARTICLE Source Type: research

Issue Information
No abstract is available for this article. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - May 17, 2020 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

A One ‐Pot Radio‐synthesis of [18F]PARPi
In this paper, we disclose a new strategy for the radio ‐synthesis of [18F]PARPi from the corresponding, boc ‐protected, nitro‐precursor. Using a two‐step procedure, [18F]PARPi could be isolated in radiochemical yields up to 9.6%. The reaction proceeds via an efficient one ‐pot, two‐step process, allowing for simplification over previous methods that require complex multi‐step, multi‐pot strategies to be implemented. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - May 11, 2020 Category: Biochemistry Authors: Thomas C. Wilson, Nagavarakishore Pillarsetty, Thomas Reiner Tags: RESEARCH ARTICLE Source Type: research

Automated Synthesis of 68Ga/177Lu ‐PSMA on the Trasis miniAllinOne
This report highlights how PSMA‐based agents for theranostic purposes can be conveniently produced at a single radiochemistry GMP‐site, thereby facilitating optimized detection and treatment of PCa. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - May 6, 2020 Category: Biochemistry Authors: Mikkel A. S ørensen, Valdemar L. Andersen, Helle Westergren Hendel, Charles Vriamont, Corentin Warnier, Julien Masset, Tri Hien Viet Huynh Tags: RESEARCH ARTICLE Source Type: research

Automated GMP production and long ‐term experience in radiosynthesis of CB1 tracer [18F]FMPEP‐d2
Here we describe the development of an in ‐house‐built device for the fully automated multi‐step synthesis of the cannabinoid CB1 receptor imaging tracer (3R,5R) ‐5‐(3‐([18F]fluoromethoxy ‐d2)phenyl) ‐3‐(((R) ‐1‐phenylethyl)amino)‐1‐(4‐(trifluoromethyl)phenyl)pyrrolidin‐2‐one ([18F]FMPEP ‐d2), following Good Manufacturing Practices. The device is interfaced to a HPLC and a sterile filtration unit in a clean room hot cell. The synthesis involves the nucleophilic18F ‐fluorination of an alkylating agent and its GC purification, the subsequent18F ‐fluoroalkylation of a precursor molecule, ...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - May 6, 2020 Category: Biochemistry Authors: Salla Lahdenpohja, Thomas Keller, Sarita Forsback, Tapio Viljanen, Esa Kokkom äki, Riikka V. Kivelä, Jörgen Bergman, Olof Solin, Anna K. Kirjavainen Tags: RESEARCH ARTICLE Source Type: research

Synthesis of stable isotope ‐labelled firocoxib
Firocoxib is a nonsteroidal, potent, and selective COX ‐2 inhibitor, approved for the control of pain and inflammation associated with osteoarthritis in dogs and horses. A six‐step synthesis was used to prepare firocoxib‐[13C6] in an overall yield of 35% from the commercially available bromobenzene ‐[13C6]. Firocoxib (ML ‐1,785,713) is a nonsteroidal, potent, and selective COX‐2 inhibitor, approved for the control of pain and inflammation associated with osteoarthritis in dogs and horses, as well as to control postoperative pain and inflammation in dogs. We employed a six‐step synthesis to prepare firocoxib...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - May 5, 2020 Category: Biochemistry Authors: Bachir Latli, Amy Gao, Valerie Kvaternick, Berhane Tecle, Scott Pennino, Nathan K. Yee, Jeff Song Tags: RESEARCH ARTICLE Source Type: research

Issue Information
No abstract is available for this article. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - May 4, 2020 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Selective synthesis of L ‐2‐[18F]fluoro‐alpha‐methylphenylalanine via copper‐mediated 18F‐fluorination of (mesityl)(aryl)iodonium salt
The first radiosynthesis of 2 ‐[18F]FAMP from18F ‐fluoride. An alpha‐methyl group substantially affected theN‐protecting group selection. These findings potentially facilitate clinical applicability of 2‐[18F]FAMP. L ‐2‐[18F]fluoro ‐alpha‐methylphenylalanine (2‐[18F]FAMP) is a promising amino acid tracer for positron emission tomography (PET) imaging, yet the low production yield of direct electrophilic radiofluorination with [18F]F2 necessitates further optimization of the radiolabeling process. This paper describes a two ‐step preparation method for L‐2‐[18F]fluoro ‐alpha‐methylphenylalanine...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - April 28, 2020 Category: Biochemistry Authors: Aiko Yamaguchi, Hirofumi Hanaoka, Tetsuya Higuchi, Yoshito Tsushima Tags: RESEARCH ARTICLE Source Type: research

S ‐(4‐Nitrobenzyl)‐6‐thioinosine: tritium labelling at high specific activity
The one step tritiation of S ‐(4‐nitrobenzyl)‐6‐thioinosine is described with characterization of the product by tritium NMR as well as mass spectrometry. The storage, stability and repurification of [benzyl methylene‐3H]S ‐(4‐nitrobenzyl)‐6‐thioinosine are also discussed. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - April 25, 2020 Category: Biochemistry Authors: Crist N. Filer, Chang Byon Tags: PROTOCOLS AND METHODS Source Type: research

A novel 99mTc ‐diester complex as tumor targeting agent: synthesis, radiolabeling and biological distribution study
The target of this study is the synthesis of a new diester derivative and radiolabeling with one of the most effective diagnostic radioisotopes to be investigated as a novel targeting radiotracer for tumor imaging. 10 ‐[2‐(9‐carboxynonanoyloxy)propoxy]‐10‐oxodecanoic acid was synthesized in excellent yield and characterized by FT‐IR, mass,1HNMR and13C ‐NMR spectra. The diester was technetium‐99m radiolabeled by direct technique using sodium dithionite as a reducing agent. The labeling parameters such as diester amount, reducing agent amount, pH of the medium and reaction time were optimized. High radiochemi...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - April 25, 2020 Category: Biochemistry Authors: Hesham A. Shamsel ‐Din, Mohamed A. Gizawy, Elsayed G. Zaki, Amr Elgendy Tags: RESEARCH ARTICLE Source Type: research

Hydrogen Isotope Exchange Labelling: a Brief Update
Journal of Labelled Compounds and Radiopharmaceuticals, Accepted Article. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - April 24, 2020 Category: Biochemistry Authors: Volker Derdau, David Hesk Tags: SPECIAL ISSUE EDITORIAL Source Type: research

Synthesis of Stable Isotope Labelled Firocoxib
Firocoxib (ML ‐1,785,713) is a nonsteroidal, potent and selective COX‐2 inhibitor, approved for the control of pain and inflammation associated with osteoarthritis in dogs and horses, as well as to control post‐operative pain and inflammation in dogs. We employed a six‐step synthesis to prepare firocoxib‐ [13C6] in an overall yield of 35% from the commercially available bromobenzene ‐13C6. The synthetic route involved the preparation of the key intermediate phenyl ‐13C6‐methyl sulfide using cesium carbonate andS ‐methylthiourea sulfate under transition ‐metal free conditions. A two‐step preparation of...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - April 19, 2020 Category: Biochemistry Authors: Bachir Latli, Amy Gao, Valerie Kvaternick, Berhane Tecle, Scott Penino, Nathan K. Yee, Jeff Song Tags: RESEARCH ARTICLE Source Type: research

Abstracts of the 27th International Isotope Society (UK group) symposium: Synthesis and applications of labelled compounds 2018
Journal of Labelled Compounds and Radiopharmaceuticals, EarlyView. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - April 6, 2020 Category: Biochemistry Tags: ABSTRACTS Source Type: research

Issue Information
No abstract is available for this article. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - April 5, 2020 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Radiosynthesis of novel N ‐18F‐labeled 18F‐FHex‐α‐l‐Glu and 18F‐FHex‐β‐Glu
Two novelN‐6‐18F ‐alkyl amino acid imaging agents,18F ‐FHex‐α‐l‐Glu and18F ‐FHex‐β‐Glu, were designed and synthesized as potential probes for PET imaging of tumors.18F ‐FHex‐α‐l‐Glu and18F ‐FHex‐β‐Glu were synthesized in decay‐uncorrected yields of 16 ± 4% (n = 5) within about 50 minutes and 11 ± 3% (n = 3) in about 60 minutes, respectively. Their radiochemical purities were more than 95%. N‐18F ‐labeled amino acids are important substitutes for new positron emission tomography (PET) imaging tracers complementing the deficiency of18F ‐fluorodeoxy...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 30, 2020 Category: Biochemistry Authors: Fuhua Wen, Shaoyu Liu, Hui Ma, Ganghua Tang Tags: RESEARCH ARTICLE Source Type: research

Arabinofuranose ‐derived positron‐emission tomography radiotracers for detection of pathogenic microorganisms
CONCLUSIONS: Arabinofuranose ‐derived18F PET radiotracers can be synthesized with high radiochemical purity. Our study showed absence of bacterial accumulation for 5 ‐substitued analogs, a finding that may have mechanistic implications for related tracers. Bothd‐2‐18F ‐AF andl‐2‐18F ‐AF showed sensitivity to most gram‐negative and gram‐positive organisms. Future in vivo studies will evaluate the diagnostic accuracy of these radiotracers in animal models of infection. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 29, 2020 Category: Biochemistry Authors: 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 Tags: RESEARCH ARTICLE Source Type: research

Nanoparticulate formulations of radiopharmaceuticals: Strategy to improve targeting and biodistribution properties
▪▪▪ Application of nanotechnology principles in drug delivery has created opportunities for treatment of several diseases. Nanotechnology offers the advantage of overcoming the adverse biopharmaceutics or pharmacokinetic properties of drug molecules, to be determined by the transport properties of the particles themselves. Through the manipulation of size, shape, charge, and type of nanoparticle delivery system, variety of distribution profiles may be obtained. However, there still exists greater need to derive and standardize definitive structure property relationships for the distribution profiles of the delivery s...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 28, 2020 Category: Biochemistry Authors: Pallab Datta, Soumendranath Ray Tags: REVIEW Source Type: research

Selective synthesis of L ‐2‐[18F]fluoro‐alpha‐methylphenylalanine via copper mediated 18F‐fluorination of (mesityl)(aryl)iodonium salt
L ‐2‐[18F]fluoro ‐alpha‐methylphenylalanine (2‐[18F]FAMP) is a promising amino acid tracer for positron emission tomography (PET) imaging, yet the low production yield of direct electrophilic radiofluorination with [18F]F2 necessitates further optimization of the radiolabeling process. This paper describes a 2 ‐step preparation method for L‐2‐[18F]fluoro ‐alpha‐methylphenylalanine (2‐[18F]FAMP) starting from [18F]fluoride.The (Mesityl)(L ‐alpha‐methylphenylalanine)‐2‐iodonium tetrafluoroborate precursors with various protecting groups were prepared. The copper‐mediated18F ‐fluorination of ...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 28, 2020 Category: Biochemistry Authors: Aiko Yamaguchi, Hirofumi Hanaoka, Tetsuya Higuchi, Yoshito Tsushima Tags: RESEARCH ARTICLE Source Type: research

Synthesis of isotopically labelled αCGRP8‐37 and its lipidated analogue
Lipidated αCGRP8 ‐37 and native αCGRP8 ‐37 are peptide antagonists of the CGRP receptor and are consequently suspected to possess antimigraine properties.13C and15N isotopically labelled variants of lipidated αCGRP8 ‐37 and native αCGRP8 ‐37 were prepared using an Fmoc solid phase peptide synthesis strategy for the purpose of the half ‐life determination.13C and15N labelled amino acids could be installed using a significantly reduced molar equivalence of activating agent and base compared to normal, whilst maintaining good coupling efficiency. α‐Calcitonin gene related peptide (&al...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 26, 2020 Category: Biochemistry Authors: Benjamin L. Lu, Kerry M. Loomes, Debbie L. Hay, Paul W.R. Harris, Margaret A. Brimble Tags: RESEARCH ARTICLE Source Type: research

Radiolabeled (R) ‐(–)‐5‐iodo‐3′‐O‐[2‐(ε‐guanidinohexanoyl)‐2‐phenylacetyl]‐2′‐deoxyuridine: A new theranostic for neuroblastoma
GPAID was designed to treat high ‐risk neuroblastoma, including relapsed or refractory disease. GPAID targets neuroblastoma cells in the same way as MIBG. It also cotargets DNA of proliferating cells, an attribute especially advantageous in the treatment ofMYCN‐amplified tumors. Neuroblastoma, the most common extracranial solid tumor in children, accounts for nearly 8% of childhood cancers in the United States. It is a disease with pronounced clinical and biological heterogeneities. The amplification ofMYCN, whose key tumorigenic functions include the promotion of proliferation, facilitation of the cell's entry into th...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 20, 2020 Category: Biochemistry Authors: Zbigniew P. Kortylewicz, Don W. Coulter, Guang Han, Janina Baranowska ‐Kortylewicz Tags: RESEARCH ARTICLE Source Type: research

Cover Image
The cover image is based on the Research ArticleA 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. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 18, 2020 Category: Biochemistry Authors: Lu Wang, Shaobo Yao, Ruikun Tang, Honghao Zhu, Lingling Zhang, Jian Gong, Qiusong Chen, Thomas Lee Collier, Hao Xu, Steven H. Liang Tags: COVER IMAGE Source Type: research

Issue Information
No abstract is available for this article. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 18, 2020 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Radiolabeled (R) ‐(–)‐5‐iodo‐3'‐O‐[2‐(ε‐guanidinohexanoyl)‐2‐phenylacetyl]‐2'‐deoxyuridine: a new theranostic for neuroblastoma
Neuroblastoma, the most common extracranial solid tumor in children, accounts for nearly 8% of childhood cancers in the United States. It is a disease with pronounced clinical and biological heterogeneities. The amplification ofMYCN, whose key tumorigenic functions include the promotion of proliferation, facilitation of the cell's entry into the S phase and prevention of cells from leaving the cell cycle, correlates with poor prognosis. Patients with a high proliferation index disease have low survival rates. Neuroblastoma is one of the most radioresponsive of all human tumors. To exploit this radiosensitivity, radioactive...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 10, 2020 Category: Biochemistry Authors: Zbigniew P. Kortylewicz, Don W. Coulter, Guang Han, Janina Baranowska ‐Kortylewicz Tags: RESEARCH ARTICLE Source Type: research

A 64Cu ‐porphyrin‐based dual‐modal molecular probe with integrin αvβ3 targeting function for tumour imaging
Pyropheophorbide ‐a (Pyro) is a promising photosensitizer for tumour photodynamictherapy (PDT) and fluorescence imaging. It is also an excellent metal chelator that can form a highly stable64Cu ‐complexes for PET imaging. However, its clinical applications are seriously restricted by poor water solubility and limited tumour targeting capability. Here, we designed a novel specific dual‐modal imaging molecular probe based on Pyro. The obtained probe64Cu ‐Pyro‐3PRGD2 has good water solubility and shows high tumour specificity in PET and optical imaging in vivo. Pyropheophorbide ‐a (Pyro) is a promising multifuncti...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 7, 2020 Category: Biochemistry Authors: Di Fan, Kai Wang, Hannan Gao, Qi Luo, Xin Wang, Xiaotong Li, Wu Tong, Xin Zhang, Chuangwei Luo, Guangjie Yang, Lin Ai, Jiyun Shi Tags: RESEARCH ARTICLE Source Type: research

Development of an automated, GMP compliant FASTlab ™ radiosynthesis of [18F]GE‐179 for the clinical study of activated NMDA receptors
We describe the development of a process using the GE FASTlab ™ radiosynthesis platform coupled with HPLC purification. The radiosynthesis is a two‐step process, involving the nucleophilic fluorination of ethylene ditosylate,11, followed by alkylation to the deprotonated thiol precursor,N‐(2‐chloro‐5‐thiophenol)‐N' ‐(3‐thiomethylphenyl)‐N' ‐methyl guanidine,8. The crude product was purified by semi ‐preparative HPLC to give the formulated product in an activity yield (AY) of 7 ± 2% (n = 15) with a total synthesis time of 120 minutes. The radioactive concentration (RAC) and radiochemical p...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - March 6, 2020 Category: Biochemistry Authors: Imtiaz Khan, Tom Christian Berg, Jane Brown, Rajiv Bhalla, Anthony Wilson, Andrew Black, Graeme McRobbie, James Nairne, Andreas Olsson, William Trigg Tags: RESEARCH ARTICLE Source Type: research

Manual vs automated 68Ga ‐radiolabelling—A comparison of optimized processes
A critical factor for clinical practice is the production of68Ga ‐radiopharmaceuticals manufactured manually or through an automated procedure.68Ga ‐radiopharmaceuticals are often prepared manually, although this method can lead to an increased operator's radiation dose and potential variability within production. The automated process is superior to manual method in all categories and presents significant improvements of68Ga ‐radiolabeling for routine clinical production in terms of reliability and reproducibility with the additional advantage of reduced operator's radiation exposure. AbstractA critical factor for c...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - February 27, 2020 Category: Biochemistry Authors: Michael Meisenheimer, Stefan K ürpig, Markus Essler, Elisabeth Eppard Tags: RESEARCH ARTICLE Source Type: research

A 64Cu ‐porphyrin based dual‐modal molecular probe with integrin αvβ3 targeting function for tumor imaging
Pyropheophorbide ‐a (Pyro) is a promising multifunctional molecule for multimodal tumor imaging and tumor photodynamic therapy (PDT), but its clinical applications are seriously restricted by the limited tumor accumulation capability. Here, we designed and synthesized a small‐molecule probe that achieved specifi c dual‐modal tumor imaging based on Pyro. Briefly, a novel molecule combining Pyro, an RGD dimer peptide (3PRGD2) and64Cu was designed and synthesized, and the obtained molecule,64Cu ‐Pyro‐3PRGD2 exhibited high tumor specificity in both positron emission tomography (PET) and optical imaging in vivo. c (RG...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - February 21, 2020 Category: Biochemistry Authors: Di Fan, Kai Wang, Hannan Gao, Qi Luo, Xin Wang, Xiaotong Li, Wu Tong, Xin Zhang, Chuangwei Luo, Guangjie Yang, Lin Ai, Jiyun Shi Tags: RESEARCH ARTICLE Source Type: research

An alternative and simple synthesis of [14C]potassium cyanate
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. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - February 14, 2020 Category: Biochemistry Authors: Crist N. Filer, C.T. Peng Tags: PRACTITIONER PROTOCOL ‐ SYNTHESIS Source Type: research

Automated radiosynthesis of [11C]UCB ‐J for imaging synaptic density by positron emission tomography
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 radiochemical yield and formulated as a 10% EtOH solution in saline with molar activities of 20 to 100 GBq/μmol. The method was based upon the palladium(0)‐mediated Suzuki cross‐coupling reaction and [11C...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - February 7, 2020 Category: Biochemistry Authors: Selena Milicevic Sephton, Tunde Miklovicz, Joseph J. Russell, Aniruddha Doke, Lei Li, Istvan Boros, Franklin I. Aigbirhio Tags: PROTOCOLS AND METHODS Source Type: research

Issue Information
No abstract is available for this article. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - February 5, 2020 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Synthesis of [3H] and [14C]Genipin
[3H]Genipin was synthesized in a single step by Ir(I) catalyzed hydrogen isotope exchange. Conditions for selective exchange of the sp2 CH bondortho to the methyl ester functionality were developed through deuterium modeling studies through a catalyst screen. Optimized conditions so obtained were then utilized with tritium gas to generate [3H]genipin at a specific activity of 18.5 Ci/mmol. Racemic [14C]genipin was prepared in 8 steps in overall 5.4% radiochemical yield from potassium [14C]cyanide. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - February 5, 2020 Category: Biochemistry Authors: A.E. Queen, D. Hesk, D.M. Lindsay, W.J. Kerr, K. Rehder, T. Fennell, W. Mascarella, D. Zhong, S. Runyon Tags: RESEARCH ARTICLE Source Type: research

Preparation of the alpha ‐emitting prostate‐specific membrane antigen targeted radioligand [212Pb]Pb‐NG001 for prostate cancer
In conclusion, the obtained results warrant further preclinical studies to evaluate the therapeutic efficacy of [212Pb]Pb ‐NG001. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 29, 2020 Category: Biochemistry Authors: Vilde Yuli Stenberg, Asta Juzeniene, Qingqi Chen, Xiaoming Yang, Øyvind Sverre Bruland, Roy Hartvig Larsen Tags: RESEARCH ARTICLE Source Type: research

Efficient radiosynthesis and preclinical evaluation of [18F]FOMPyD as a positron emission tomography tracer candidate for TrkB/C receptor imaging
Efficient radiosynthesis of [18F]FOMPyD in one concerted copper ‐mediated step and its preclinical investigation as a putative dual Trk/CSF‐1R PET tracer Herein we report an efficient radiolabeling of a18F ‐fluorinated derivative of dual inhibitor GW2580, with its subsequent evaluation as a positron emission tomography (PET) tracer candidate for imaging of two neuroreceptor targets implicated in the pathophysiology of neurodegeneration: tropomyosin receptor kinases (TrkB/C) and colony stimulating fa ctor receptor (CSF‐1R). [18F]FOMPyD was synthesized from a boronic acid pinacolate precursorvia copper ‐mediated18F...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 29, 2020 Category: Biochemistry Authors: Thomas A. Singleton, Hussein Bdair, Justin J. Bailey, Sangho Choi, Arturo Aliaga, Pedro Rosa ‐Neto, Ralf Schirrmacher, Vadim Bernard‐Gauthier, Alexey Kostikov Tags: RESEARCH ARTICLE Source Type: research

Development of an automated, GMP compliant FASTlabTM radiosynthesis of [18F]GE ‐179 for the clinical study of activated NMDA receptors
We describe the development of a process using the GE FASTlabTM radiosynthesis platform coupled with HPLC purification. The radiosynthesis is a two ‐step process, involving the nucleophilic fluorination of ethylene ditosylate, 11, followed by alkylation to the deprotonated thiol precursor,N‐(2‐chloro‐5‐thiophenol)‐N’‐(3‐thiomethylphenyl)‐N’‐methyl guanidine, 8.The crude product was purified by semi ‐preparative HPLC to give the formulated product in an activity yield (AY) of 7 ± 2% (n = 15) with a total synthesis time of 120 minutes. The radioactive concentration (RAC) and radiochem...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 27, 2020 Category: Biochemistry Authors: Imtiaz Khan, Tom Christian Berg, Jane Brown, Rajiv Bhalla, Anthony Wilson, Andrew Black, Graeme McRobbie, James Nairne, Andreas Olsson, William Trigg Tags: RESEARCH ARTICLE Source Type: research

Issue Information
No abstract is available for this article. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 23, 2020 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Synthesis of imatinib, a tyrosine kinase inhibitor, labeled with carbon ‐14
In this study, we report the synthetic optimization for14C ‐labeling and radiosynthesis of [14C]imatinib to analyze binding with cellular proteins using accelerator mass spectroscopy (AMS).14C ‐labeling of imatinib was performed by the synthesis of14C ‐labeld 2‐aminopyrimidine intermediate using [14C]guanidine ·HCl, which includes anin ‐situ reduction of an inseparable byproduct for easy purification by HPLC, followed by a cross ‐coupling reaction with aryl bromide precursor. The radiosynthesis of [14C]imatinib (specific activity, 631 MBq/mmol; radiochemical purity, 99.6%) was achieved in six steps with ...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 23, 2020 Category: Biochemistry Authors: Julie Kang, Jun Young Lee, Jeong ‐Hoon Park, Dong‐Jo Chang Tags: RESEARCH ARTICLE Source Type: research

“In‐loop” carbonylation—A simplified method for carbon‐11 labelling of drugs and radioligands
A new “in‐loop” methodology was developed to simplify palladium‐mediated carbonylations with [11C]carbon monoxide. The methodology proved to be useful in generating11C ‐labelled amides, esters and carboxylic acids. Given its simplicity, efficiency and compatibility with automation, this methodology may become a valuable addition to the toolbox of methodologies used for11C ‐carbonylation of drugs and radioligands for PET. AbstractTransition ‐metal mediated carbonylation with11C ‐labelled carbon monoxide ([11C]CO) is a versatile method for introducing11C (t1/2 = 20.3 min) into drugs and radioligands f...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 21, 2020 Category: Biochemistry Authors: M élodie Ferrat, Kenneth Dahl, Christer Halldin, Magnus Schou Tags: RESEARCH ARTICLE Source Type: research

A concisely automated synthesis of TSPO radiotracer [18F]FDPA based on spirocyclic iodonium ylide method and validation for human use
The present study reports a successful one ‐step radiolabeling of fluorine‐18 labeledN,N‐diethyl‐2‐(2‐(4‐(2‐fluoroethoxy)phenyl)‐5,7‐dimethylpyrazolo[1,5‐a]pyrimidin ‐3‐yl)acetamide ([18F]FDPA) on a GE TRACERlab FX2 N synthesis module with a novel spirocyclic iodonium ylide (SCIDY) precursor, which has demonstrated the highest radiochemical yields and molar activity from [18F]fluoride ion. This protocol has been validated for human use. Fluorine ‐18 labeledN,N‐diethyl‐2‐(2‐(4‐(2‐fluoroethoxy)phenyl)‐5,7‐dimethylpyrazolo[1,5‐a]pyrimidin ‐3‐yl)acetamide ([18F]FDPA) is a poten...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 20, 2020 Category: Biochemistry Authors: Lu Wang, Shaobo Yao, Ruikun Tang, Honghao Zhu, Lingling Zhang, Jian Gong, Qiusong Chen, Thomas Lee Collier, Hao Xu, Steven H. Liang Tags: RESEARCH ARTICLE Source Type: research

Base Metal ‐Catalyzed Hydrogen Isotope Exchange
Hydrogen isotope exchange (HIE) has played an increasingly important role in deuteration and tritiation of compounds in the pharmaceutical industry. Transition metal ‐catalyzed HIE methods have gained considerable attention in the past decades, and most of these methods were comprehensively reviewed in 2010 in a special JLCR issue. It covered a wide variety of HIE catalysis systems involving precious metal catalysts, and a relatively small percentage of base m etal catalysts, with a major focus on heterogeneous nickel. While base metal catalysts have remained under‐developed for HIE chemistry relative to 2nd and 3rd ro...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 16, 2020 Category: Biochemistry Authors: Haifeng Yang, David Hesk Tags: SPECIAL ISSUE REVIEW Source Type: research

Comparison of biological properties of [177Lu]Lu ‐ProBOMB1 and [177Lu]Lu‐NeoBOMB1 for GRPR targeting
A lutetium bombesin derivative targeting the gastrin ‐releasing peptide receptor was evaluated in a model of prostate cancer. Our data suggests that the selection of radiometal can adversely affect tumor uptake and pharmacokinetics of ProBOMB1. AbstractThe gastrin ‐releasing peptide receptor (GRPR) is overexpressed in prostate cancer and other solid malignancies. Following up on our work on [68Ga]Ga ‐ProBOMB1 that had better imaging characteristics than [68Ga]Ga ‐NeoBOMB1, we investigated the effects of substituting68Ga for177Lu to determine if the resulting radiopharmaceuticals could be used with a therapeutic aim...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 11, 2020 Category: Biochemistry Authors: Etienne Rousseau, Joseph Lau, Zhengxing Zhang, Chengcheng Zhang, Daniel Kwon, Carlos F. Uribe, Hsiou ‐Ting Kuo, Jutta Zeisler, Ivica Bratanovic, Kuo‐Shyan Lin, François Bénard Tags: RESEARCH ARTICLE Source Type: research

Radiosynthesis and preliminary evaluation of an 18F ‐labeled tubastatin A analog for PET imaging of histone deacetylase 6
Histone deacetylase 6 (HDAC6), a unique member of the HDAC family, has been implicated in cancers and neurodegenerative diseases. An18F ‐labeled analog of tubastatin A was synthesized for PET imaging of HDAC6, and a preliminary biological evaluation was performed. AbstractHistone deacetylase 6 (HDAC6) is a unique member of the HDAC family because of its characteristics, namely, its cytoplasmic localization and ubiquitin binding. HDAC6 has been implicated in cancer metastasis and neurodegeneration. In the present study, we performed radiosynthesis and biological evaluation of a fluorine ‐18–labeled ligand [18F]3, ...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 9, 2020 Category: Biochemistry Authors: Tetsuro Tago, Jun Toyohara, Kenji Ishii Tags: RESEARCH ARTICLE Source Type: research

Preparation of the alpha ‐emitting PSMA targeted radioligand [212Pb]Pb‐NG001 for prostate cancer
In conclusion, the obtained results warrant further preclinical studies to evaluate the therapeutic efficacy of [212Pb]Pb ‐NG001. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 9, 2020 Category: Biochemistry Authors: Vilde Yuli Stenberg, Asta Juzeniene, Qingqi Chen, Xiaoming Yang, Øyvind Sverre Bruland, Roy Hartvig Larsen Tags: RESEARCH ARTICLE Source Type: research

Efficient radiosynthesis and preclinical evaluation of [18F]FOMPyD as a PET tracer candidate for TrkB/C receptor imaging
Herein we report an efficient radiolabeling of a18F ‐fluorinated derivative of dual inhibitor GW2580, with its subsequent evaluation as a positron emission tomography (PET) tracer candidate for imaging of two neuroreceptor targets implicated in the pathophysiology of neurodegeneration: tropomyosin receptor kinases (TrkB/C) and colony stimulating fa ctor receptor (CSF‐1R). [18F]FOMPyD was synthesized from a boronic acid pinacolate precursorvia copper ‐mediated18F ‐fluorination concerted with thermal deprotection of the four Boc groups on a diaminopyrimidine moiety in an 8.7±2.8% radiochemical yield, a radioch...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 9, 2020 Category: Biochemistry Authors: Thomas A. Singleton, Hussein Bdair, Justin J. Bailey, Sangho Choi, Arturo Aliaga, Pedro Rosa ‐Neto, Ralf Schirrmacher, Vadim Bernard‐Gauthier, Alexey Kostikov Tags: RESEARCH ARTICLE Source Type: research

Radiosynthesis of the 11C ‐methyl derivative of LBQ657 for PET investigation of the neprilysin inhibitor sacubitril
[11C]MeOLBQ was produced from [11C]methyl triflate followed by the deprotection of the tertbutylester in acidic conditions. Neprilysin, also known as neutral endopeptidase, is a cell surface membrane metalo ‐endopeptidase that cleaves various peptides. Altered neprilysin expression has been correlated with various cancers and cardiovascular diseases. In this work, we present the radiosynthesis of the novelO‐11C ‐methylated derivative of LBQ657 (a potent neprilysin inhibitor). (2R,4S) ‐5‐(Biphenyl‐4‐yl)‐4‐[(3‐carboxypropionyl)amino]‐2‐methylpentanoic acid [11C]methyl ester ([11C]MeOLBQ) is an analog ...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 8, 2020 Category: Biochemistry Authors: Valentin R. Teyssier, Jos é‐Mathieu Simard, Mark H. Dornan, François Tournoux, Jean N. DaSilva Tags: RESEARCH ARTICLE Source Type: research

A concisely automated synthesis of TSPO radiotracer [18F]FDPA based on spirocyclic iodonium ylide (SCIDY) method and validation for human use
Fluorine ‐18 labeledN,N‐diethyl‐2‐(2‐(4‐(2‐fluoroethoxy)phenyl)‐5,7‐dimethylpyrazolo[1,5‐a]pyrimidin ‐3‐yl)acetamide ([18F]FDPA) is a potent and selective radiotracer for PET imaging of the translocator protein 18 kDa (TSPO). Our previousin vitro andin vivo evaluations have proven that this tracer is promising for further human translation. Our study addresses the need to streamline the automatic synthesis of this radiotracer to make it more accessible for widespread clinical evaluation and application. Here, we successfully demonstrate a one ‐step radiolabeling of [18F]FDPA based on a novel spiro...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - January 2, 2020 Category: Biochemistry Authors: Lu Wang, Shaobo Yao, Ruikun Tang, Honghao Zhu, Lingling Zhang, Jian Gong, Qiusong Chen, Thomas Lee Collier, Hao Xu, Steven H. Liang Tags: RESEARCH ARTICLE Source Type: research

Tetrabutylammonium HPLC analysis: shortcomings in the Ph. Eur. method
Tetrabutylammonium is a phase ‐transfer agent commonly used in PET radiochemistry. Its toxicity makes its quantification mandatory. However, the official HPLC method for tetrabutylammonium analysis reported in the European Pharmacopoeia (Ph. Eur.) apparently fails to achieve the described separation in most new generation reve rse‐phase columns. The study highlights the differences in separation achievable by varying some of the chromatographic conditions, such as temperature, eluent composition and ion‐pairing agent concentration. In the end, variations to the method within the limits allowed by the Ph. Eur. were no...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - December 30, 2019 Category: Biochemistry Authors: Anna Bogni, Claudio Cucchi, Luca Laera, Ettore Cesare Seregni, Claudio Pascali Tags: NOTE Source Type: research

Radiosynthesis and preliminary evaluation of an 18F ‐labeled Tubastatin A analogue for PET imaging of histone deacetylase 6
Histone deacetylase 6 (HDAC6) is a unique member of the HDAC family because of its characteristics, namely its cytoplasmic localization and ubiquitin binding. HDAC6 has been implicated in cancer metastasis and neurodegeneration. In the present study, we performed radiosynthesis and biological evaluation of a fluorine ‐18‐labeled ligand [18F]3, which is an analogue of the HDAC6 ‐selective inhibitor Tubastatin A, for PET imaging. [18F]3 was synthesized by a two ‐step reaction composed of18F ‐fluorination and formation of a hydroxamic acid group. IC50 values of3 against HDAC1 and HDAC6 activities were 996 and 33.1 n...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - December 27, 2019 Category: Biochemistry Authors: Tetsuro Tago, Jun Toyohara, Kenji Ishii Tags: RESEARCH ARTICLE Source Type: research

Issue Information
No abstract is available for this article. (Source: Journal of Labelled Compounds and Radiopharmaceuticals)
Source: Journal of Labelled Compounds and Radiopharmaceuticals - December 20, 2019 Category: Biochemistry Tags: ISSUE INFORMATION Source Type: research

Manual vs. automated 68Ga ‐radiolabeling ‐ a comparison of optimized processes
A critical factor for clinical practice is the production of68Ga ‐radiopharmaceuticals manufactured manually or through an automated procedure.68Ga ‐radiopharmaceuticals are often prepared manually, although this method can lead to an increased operator´s radiation dose and potential variability within production.The present work compares68Ga ‐radiolabeling (PSMA‐11; DOTA‐TOC) utilizing a cassette module (GAIA; Elysia‐Raytest; Germany) with a manual setup for routine clinical production with regard to process reliability and reproducibility.A total 837 routine production batches from 2015 ‐2017 were ret...
Source: Journal of Labelled Compounds and Radiopharmaceuticals - December 16, 2019 Category: Biochemistry Authors: Michael Meisenheimer, Stefan K ürpig, Markus Essler, Elisabeth Eppard Tags: RESEARCH ARTICLE Source Type: research